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Publications and Presentations Featuring TAACF Research



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Categories:

  • Compounds and Compound Series in Clinical Trials

  • Compounds Evaluated In Vivo

  • Methods Development

  • Biochemical Targets and HTS Assays

  • Priority Compounds
     
  • Reviews and Summaries of TAACF Actives

  • Compounds with In Vitro Data




Compounds and Compound Series in Clinical Trials

  1. Hu, Y.; Coates, A. R.; Mitchison, D. A. Sterilizing activities of fluoroquinolones against rifampin-tolerant populations of Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 2003, 47 (2), 653-657.

  2. Lenaerts, A. J.; Marietta, K. S.; Gruppo, V.; Johnson, J.; Near, K. A.; Laughon, B. E.; Rouse, D.; Orme, I.  Efficacy of the Nitroimidazopyran PA-824 in Tuberculosis Animal Models. ICAAC meeting, Washington DC . 2004.

Ref Type: Abstract

  3. Lenaerts, A. J.; Gruppo, V.; Marietta, K. S.; Johnson, C. M.; Driscoll, D. K.; Tompkins, N. M.; Rose, J. D.; Reynolds, R. C.; Orme, I. M. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob. Agents Chemother. 2005, 49 (6), 2294-2301.

  4. Lenaerts, A. J.; Gruppo, V.; Marietta, K. S.; Johnson, C. M.; Orme, I. M.  Preclinical Testing of the quinolone KRQ-10018 for Activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy, San Francisco, CA . 9-29-2006.

Ref Type: Abstract

  5. Lenaerts, A. J.; Lasco, T.; Cantarero, L.; Sahar, A.; Ehlers, S.; Andries, K.; Orme, I.; Basaraba, R.  Location of persisting mycobacteria in the guinea pig model of tuberculosis revealed by R207910. Keystone Symposia - Tuberculosis: From Lab Research to field trials.  2007.

Ref Type: Abstract

  6. Protopopova, M.; Hanrahan, C.; Nikonenko, B.; Samala, R.; Chen, P.; Gearhart, J.; Einck, L.; Nacy, C. A. Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines. J. Antimicrob. Chemother. 2005, 56 (5), 968-974

Compounds Evaluated In Vivo

  1. Bakkestuen, A. K.; Gundersen, L. L.; Utenova, B. T. Synthesis, biological activity, and SAR of antimycobacterial 9-aryl-, 9-arylsulfonyl-, and 9-benzyl-6-(2-furyl)purines. J. Med Chem 2005, 48 (7), 2710-2723.

  2. Bermudez, L. E.; Reynolds, R.; Kolonoski, P.; Aralar, P.; Inderlied, C. B.; Young, L. S. Thiosemicarbazole (thiacetazone-like) compound with activity against Mycobacterium avium in mice. Antimicrob. Agents Chemother. 2003, 47 (8), 2685-2687.

  3. Bermudez, L. E.; Kolonoski, P.; Seitz, L. E.; Petrofsky, M.; Reynolds, R.; Wu, M.; Young, L. S. SRI-286, a thiosemicarbazole, in combination with mefloquine and moxifloxacin for treatment of murine Mycobacterium avium complex disease. Antimicrob. Agents Chemother. 2004, 48 (9), 3556-3558.

  4. Centrone, C. A.; Lowary, T. L. Synthesis and antituberculosis activity of C-phosphonate analogues of decaprenolphosphoarabinose, a key intermediate in the biosynthesis of mycobacterial arabinogalactan and lipoarabinomannan. J. Org. Chem 2002, 67 (25), 8862-8870.

  5. Hearn, M. J.; Cynamon, M. H. In vitro and in vivo activities of acylated derivatives of isoniazid against mycobacterium tuberculosis. Drug Des Discov. 2003, 18 (4), 103-108.

  6. Johnson, C. M.; Pandey, R.; Sharma, S.; Khuller, G. K.; Basaraba, R. J.; Orme, I. M.; Lenaerts, A. J. Oral therapy using nanoparticle-encapsulated antituberculosis drugs in guinea pigs infected with Mycobacterium tuberculosis. Antimicrob. Agents Chemother.  2005, 49 (10), 4335-4338.

  7. Lenaerts, A. J.; Chapman, P. L.; Orme, I. M. Statistical limitations to the Cornell model of latent tuberculosis infection for the study of relapse rates. Tuberculosis. (Edinb. ) 2004, 84 (6), 361-364.

  8. Lenaerts, A. J.; Johnson, C. M.; Marrieta, K. S.; Gruppo, V.; Orme, I. M. Significant increases in the levels of liver enzymes in mice treated with anti-tuberculosis drugs. Int. J. Antimicrob. Agents 2005, 26 (2), 152-158.

  9. Lenaerts, A. J.; Gruppo, V.; Johnson, C.; Marietta, K.; Driscoll, D.; Tompkin, N.; Near, K. A.; Laughon, B.; Orme, I. M.  Promising compound series with activity in animal models of tuberculosis. US Japan - 14th Tuberculosis and Leprosy Research Conference, Seattle, WA . 2005.

Ref Type: Abstract

10. Lenaerts, A. J.  "Promising compound series with activity in animal models of tuberculosis". TB 2006 Meeting, Gambia, West-Africa . 2006.

Ref Type: Abstract

11. Sriram, D.; Yogeeswari, P.; Basha, J. S.; Radha, D. R.; Nagaraja, V. Synthesis and antimycobacterial evaluation of various 7-substituted ciprofloxacin derivatives. Bioorg. Med Chem 2005, 13 (20), 5774-5778.

Methods Development

  1. Cho, S. H.; Warit, S.; Wan, B.; Hwang, C. H.; Pauli, G. F.; Franzblau, S. G. Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 2007, 51 (4), 1380-1385.

  2. Collins, L.; Franzblau, S. G. Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium. Antimicrob. Agents Chemother. 1997, 41 (5), 1004-1009.

  3. Franzblau, S. G.; Witzig, R. S.; McLaughlin, J. C.; Torres, P.; Madico, G.; Hernandez, A.; Degnan, M. T.; Cook, M. B.; Quenzer, V. K.; Ferguson, R. M.; Gilman, R. H. Rapid, low-technology MIC determination with clinical Mycobacterium tuberculosis isolates by using the microplate Alamar Blue assay. J. Clin Microbiol. 1998, 36 (2), 362-366.

  4. Gruppo, V.; Marietta, K.; Johnson, C. M.; Adams, L.; Orme, I. M.; Lenaerts, A. J.  Rapid evaluation of novel compounds against tuberculosis. Japan - 14th Tuberculosis and Leprosy Research Conference, Seattle, WA. 2005.

Ref Type: Abstract

  5. Gruppo, V.; Johnson, C. M.; Marietta, K. S.; Scherman, H.; Zink, E. E.; Crick, D. C.; Adams, L. B.; Orme, I. M.; Lenaerts, A. J. Rapid microbiologic and pharmacologic evaluation of experimental compounds against Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 2006, 50 (4), 1245-1250.

  6. Lenaerts, A. J.; Gruppo, V.; Orme, I. M.  Models for identifying potential drug candidates for latent tuberculosis. 102nd General ASM meeting. 2002.

Ref Type: Abstract

  7. Lenaerts, A. J.; Gruppo, V.; Brooks, J. V.; Orme, I. M. Rapid in vivo screening of experimental drugs for tuberculosis using gamma interferon gene-disrupted mice. Antimicrob. Agents Chemother. 2003, 47 (2), 783-785.

  8. Lenaerts, A. J.  A State-of-the-Art Minilecture: "Animal Models of Antituberculosis Therapy and the Effect of the Host Immune Response". 45th Interscience Conference on Antimicrobial Agents and Chemotherapy, Washington DC. 12-17-2005.

Ref Type: Abstract

Biochemical Targets and HTS Assays

  1. Anathan, A.; Biswas, A.; Fletcher III, T. M.; Franzblau, S.; Guthrie, T.; Krahenbuhl, J.; Kwaon, C.; Laughon, B.; Lenaerts, A.; Maddry, J.; Michael, M.; Poffenberger, A.; Secrist, J. A.; Suling, W. J.  Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) Program:  High Throughput Primary and Target Based Mycobacterium tuberculosis Screening. Society for Biomolecular Sciences (SBS) 8th annual conference, The Hague, The Netherlands . 2002.

Ref Type: Abstract

  2. Collins, L. A.; Torrero, M. N.; Franzblau, S. Green fluorescent protein reporter microplate assay for high-throughput screening of compounds against Mycobacterium tuberculosis. Antimicrob. Agents Chemother. 1998, 42 (2), 344-347.

  3. Cooley, S.; Southworth, K.; Ross, L.; Reddy, L.; Gray, R.; Sosa, M. I.; Manouvakhova, A.; Feng, S.; Maddox, C.; Rasmussen, L.; White, E. L.; Anathan, A.; Fletcher III, T. M.; Goldman, R. C.; Sacchettini, J.  A High Throughput Screening Assay for Malate Synthase Inhibitors of Mycobacterium tuberculosis. Society for Biomolecular Sciences (SBS) 12th annual conference, Seattle, USA . 2006.

Ref Type: Abstract

  4. Fletcher III, T. M.; Gill, R.; Drummond, T.; White, E. L.; Valiyaveettil, J.; Bittman, R.; Kuo, M.; Sacchettini, J.; Jacobs Jr, W. R.  A High Throughput Screen for the Mycobacterium Tuberculosis Enoyl Acyl Carrier Protein Reductase, InhA. Society for Biomolecular Sciences (SBS) 9th annual conference, Portland, USA . 2003.

Ref Type: Abstract

  5. Gill, R.; Ross, L.; Cooley, S.; Pate, A.; Manouvakhova, A.; Lampl, M.; Barnett, D.; White, E. L.; Sacchettini, J.; Fletcher III, T. M.  A High Throughput Screening Assay for Inhibitors of Mycobacterium tuberculosis Enoyl ACP Reductase (InhA). Society for Biomolecular Sciences (SBS) 10th annual conference, Orlando, USA . 2004.

Ref Type: Abstract

  6. Gill, R.; Drummond, T.; Escuyer, V.; Ingrum, M.; Ross, L.; White, E. L.; Suling, W. J.; Fletcher III, T. M.  An Automated High Throughput Screen for Dihydrofolate Reductase Using Catalytic Reduction of MTS to Identify Inhibitors of Mycobacterium tuberculosis. Society for Biomolecular Sciences (SBS) 9th annual conference, Portland, USA . 2007.

Ref Type: Abstract

  7. Guthrie, T.; Bradford, P.; Escuyer, V.; Fiedler, J.; Ingrum, M.; Poe, A.; Rizvi, A.; Ross, L.; White, E. L.; Suling, W. J.; Fletcher III, T. M.  Development and Evaluation of High Throughput Screening for Dihydrofolate Reductase Enzyme Inhibition Assays for Mycobacterium tuberculosis. 4th World Congress on Tuberculosis, Washington, D.C., USA . 2002.

Ref Type: Abstract

  8. Guthrie, T.; Rizvi, A.; Bradford, P.; Ingrum, M.; Fiedler, J.; Escuyer, V.; White, E. L.; Suling, W. J.; Fletcher III, T. M.  Development and Automation of a High Throughput Screen for Dihydrofolate Reductase Enzyme Inhibition Assays for Mycobacterium tuberculosis. Society for Biomolecular Sciences (SBS) 8th annual conference, The Hague, The Netherlands . 2006.

Ref Type: Abstract

  9. Kushner, N.; Southworth, K.; Minyard, M. B.; Cooley, S.; Lampl, M.; Sosa, M. I.; Pate, A.; Manouvakhova, A.; Suling, W. J.; Escuyer, V.; Fletcher III, T. M.  A Fluorescence-Based High Throughput Screen for Inhibitors of Mycobacterium tuberculosis. Society for Biomolecular Sciences (SBS) 10th annual conference, Orlando, USA . 2004.

Ref Type: Abstract

10. Kushner, N.; Severson, W.; Pate, A.; Shindo, N.; Rasmussen, L.; Johnson, C.; White, E. L.  High Throughput Screening With Infectious Agents:  Equipment Choices and Strategies. Lab Automation 10th annual conference, Palm Springs, USA . 2007.

Ref Type: Abstract

11. Madison-Antenucci, S.; Ross, L.; White, E. L.; Fletcher III, T. M.  Measurement of Fluorescent FtsZ from Mycobacterium tuberculosis in a High-Throughput Assay. Society for Biomolecular Sciences (SBS) 9th annual conference, Portland, USA . 2007.

Ref Type: Abstract

12. Minyard, M. B.; Southworth, K.; Suling, W. J.; Ingrum, M.; Pate, A.; Escuyer, V.; Fletcher III, T. M.  Automation and Validation of a Fluorescent-Based High Throughput Screen for Inhibitors of Mycobacterium Tuberculosis. Society for Biomolecular Sciences (SBS) 9th annual conference, Portland, USA . 2003.

Ref Type: Abstract

13. Sneed, B.; Ross, L.; Sosa, M. I.; Cooley, S.; Pate, A.; Manouvakhova, A.; Barnett, D.; White, E. L.; Wang, S.; Esenberg, D.; Goulding, C.; Fletcher III, T. M.  A High Throughput Screening Assay for Pantothenate Synthetase Inhibitors of Mycobacterium tuberculosis.   Society for Biomolecular Sciences (SBS) 10th annual conference, Orlando, USA . 2004.

Ref Type: Abstract

14. Sneed, B.; van-Ginkel, S.; Gill, R.; Ross, L.; Sosa, M. I.; Cooley, S.; Pate, A.; Manouvakhova, A.; Lampl, M.; Barnett, D.; White, E. L.; Sacchettini, J.; Fletcher III, T. M.  A High Throughput Screening Assay for Isocitrate Lyase Inhibitors of Mycobacterium tuberculosis. Society for Biomolecular Sciences (SBS) 10th annual conference, Orlando, USA . 2004.

Ref Type: Abstract

15. Southworth, K.; Sneed, B.; Ross, L.; Cooley, S.; Sosa, M. I.; Manouvakhova, A.; Rasmussen, L.; White, E. L.; Anathan, A.; Fletcher III, T. M.; Goldman, R. C.; Goulding, C.; Eisenberg, D.  Identifying Pantothenate Synthetase Inhibitors of Mycobacterium tuberculosis from a High Throughput Screen. Society for Biomolecular Sciences (SBS) 13th annual conference, Montreal, Canada . 2007.

Ref Type: Abstract

16. White, E. L.; Southworth, K.; Ross, L.; Cooley, S.; Gill, R. B.; Sosa, M. I.; Manouvakhova, A.; Rasmussen, L.; Goulding, C.; Eisenberg, D.; Fletcher, T. M., III A novel inhibitor of Mycobacterium tuberculosis pantothenate synthetase. J. Biomol. Screen. 2007, 12 (1), 100-105.

Priority Compounds

  1. Andreani, A.; Granaiola, M.; Leoni, A.; Locatelli, A.; Morigi, R.; Rambaldi, M. Synthesis and antitubercular activity of imidazo[2,1-b]thiazoles. Eur. J. Med. Chem. 2001, 36 (9), 743-746.

  2. Ates, O.; Altintas, H.; Otuk, G. Synthesis and antimicrobial activity of 4-carbethoxymethyl-2-[(alpha-haloacyl)amino] thiazoles and 5-nonsubstituted/substituted 2-[(4-carbethoxymethylthiazol-2-yl)imino]-4-thiazolidinones. Arzneimittelforschung. 2000, 50 (6), 569-575.

  3. Badawneh, M.; Manera, C.; Mori, C.; Saccomanni, G.; Ferrarini, P. L. Synthesis of variously substituted 1,8-naphthyridine derivatives and evaluation of their antimycobacterial activity. Il Farmaco 2002, 57 (8), 631-639.

  4. Badawneh, M.; Bellini, L.; Cavallini, T.; Al-jamal J.; Manera, C.; Saccomanni, G.; Ferrarini, P. L. Synthesis of 3- or 4-phenyl-1,8-naphthyridine derivatives and evaluation of antimycobacterial and antimicrobial activity. Farmaco 2003, 58 (9), 859-866.

  5. Bhowruth, V.; Brown, A. K.; Reynolds, R. C.; Coxon, G. D.; Mackay, S. P.; Minnikin, D. E.; Besra, G. S. Symmetrical and unsymmetrical analogues of isoxyl; active agents against Mycobacterium tuberculosis. Bioorg. Med. Chem. Lett. 2006, 16 (18), 4743-4747.

  6. Bottari, B.; Maccari, R.; Monforte, F.; Ottana, R.; Rotondo, E.; Vigorita, M. G. Antimycobacterial in vitro activity of cobalt(II) isonicotinoylhydrazone complexes. Part 10. Bioorg. Med. Chem. Lett. 2001, 11 (3), 301-303.

  7. Carta, A.; Paglietti, G.; Rahbar Nikookar, M. E.; Sanna, P.; Sechi, L.; Zanetti, S. Novel substituted quinoxaline 1,4-dioxides with in vitro antimycobacterial and anticandida activity. Eur. J. Med. Chem. 2002, 37 (5), 355-366.

  8. Dolezal, M.; Miletin, M.; Kunes, J.; Kralova, K. Substituted amides of pyrazine-2-carboxylic acids, their synthesis and biological activity. Molecules 2002, 7, 363-373.

  9. Dolezal, M.; Jampilek, J.; Osicka, Z.; Kunes, J.; Buchta, V.; Vichova, P. Substituted 5-aroylpyrazine-2-carboxylic acid derivatives: synthesis and biological activity. Farmaco 2003, 58 (11), 1105-1111.

10. Dolezal, M.; Palek, L.; Vinsova, J.; Buchta, V.; Jampilek, J.; Kralova, K. Substituted pyrazinecarboxamides: Synthesis and biological evaluation. Molecules 2006, 11 (4), 242-256.

11. Foroumadi, A.; Mirzaei, M.; Shafiee, A. Antituberculosis agents, I: Synthesis and antituberculosis activity of 2-aryl-1,3,4-thiadiazole derivatives. Pharmazie 2001, 56 (8), 610-612.

12. Foroumadi, A.; Soltani, F.; Rezaee, M. A.; Moshafi, M. H. Synthesis and evaluation of in vitro antimycobacterial activity of some 5-(5-nitro-2-thienyl)-2-(piperazinyl, piperidinyl and morpholinyl)-1,3,4-thiadiazole derivatives. Boll. Chim. Farm. 2003, 142 (9), 416-419.

13. Foroumadi, A.; Soltani, F.; Jabini, R.; Moshafi, M. H.; Rasnani, F. M. Antituberculosis agents X. Synthesis and evaluation of in vitro antituberculosis activity of 2-(5-nitro-2-furyl)- and 2-(1-methyl-5-nitro-1H-imidazol-2-yl)-1,3,4-thiadiazole derivatives. Arch. Pharm. Res. 2004, 27 (5), 502-506.

14. Foroumadi, A.; Soltani, F.; Moallemzadeh-Haghighi, H.; Shafiee, A. Synthesis, in vitro-antimycobacterial activity and cytotoxicity of some alkyl alpha-(5-aryl-1, 3, 4-thiadiazole-2-ylthio)acetates. Arch. Pharm. (Weinheim) 2005, 338 (2-3), 112-116.

15. Foroumadi, A.; Kargar, Z.; Sakhteman, A.; Sharifzadeh, Z.; Feyzmohammadi, R.; Kazemi, M.; Shafiee, A. Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio]propionates. Bioorg. Med. Chem. Lett. 2006, 16 (5), 1164-1167.

16. Guillon, J.; Reynolds, R. C.; Leger, J. M.; Guie, M. A.; Massip, S.; Dallemagne, P.; Jarry, C. Synthesis and preliminary in vitro evaluation of antimycobacterial activity of new pyrrolo[1,2-a] quinoxaline-carboxylic acid hydrazide derivatives. J. Enzyme Inhib. Med. Chem. 2004, 19 (6), 489-495.

17. Gursoy, A.; Karali, N. 4-(3-coumarinyl)-4-thiazolin-2-one benzylidenehydrazones with antituberculosis activity. Arzneimittelforschung. 2000, 50 (2), 167-172.

18. Guzel, O.; Salman, A. Synthesis, antimycobacterial and antitumor activities of new (1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methyl N,N-disubstituted dithiocarbamate/O-alkyldithiocarbonate derivatives. Bioorg. Med Chem 2006, 14 (23), 7804-7815.

19. He, X.; Alian, A.; Stroud, R.; Ortiz de Montellano, P. R. Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis. J. Med Chem 2006, 49 (21), 6308-6323.

20. Imamura, P. M.; Costa, M. Synthesis of 16,18-dihydroxycleroda-3,13Z-dien-16,15-olide, (+)-16-hydroxycleroda-3,13Z-dien-16,15-olide, and (-)-hydroxyhalima-5(10),13-dien-16,15-olide from (+)-hardwickiic acid. J. Nat Prod. 2000, 63 (12), 1623-1625.

21. Jaso, A.; Zarranz, B.; Aldana, I.; Monge, A. Synthesis of new 2-acetyl and 2-benzoyl quinoxaline 1,4-di-N-oxide derivatives as anti-Mycobacterium tuberculosis agents. Eur. J. Med. Chem. 2003, 38 (9), 791-800.

22. Jaso, A.; Zarranz, B.; Aldana, I.; Monge, A. Synthesis of new quinoxaline-2-carboxylate 1,4-dioxide derivatives as anti-Mycobacterium tuberculosis agents. J. Med. Chem 2005, 48 (6), 2019-2025.

23. Koketsu, M.; Tanaka, K.; Takenaka, Y.; Kwong, C. D.; Ishihara, H. Synthesis of 1,3-thiazine derivatives and their evaluation as potential antimycobacterial agents. Eur. J. Pharm. Sci. 2002, 15 (3), 307-310.

24. Krinkova, J.; Dolezal, M.; Hartl, J.; Buchta, V.; Pour, M. Synthesis and biological activity of 5-alkyl-6-(alkylsulfanyl)- or 5-alkyl-6-(arylsulfanyl)pyrazine-2-carboxamides and corresponding thioamides. Farmaco 2002, 57 (1), 71-78.

25. Kucukguzel, I.; Kucukguzel, S. G.; Rollas, S.; Kiraz, M. Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials. Bioorg. Med. Chem. Lett. 2001, 11 (13), 1703-1707.

26. Kucukguzel, I.; Guniz, K. S.; Rollas, S.; Otuk-Sanis, G.; Ozdemir, O.; Bayrak, I.; Altug, T.; Stables, J. P. Synthesis of some 3-(arylalkylthio)-4-alkyl/aryl-5-(4-aminophenyl)-4H-1,2,4-triazole derivatives and their anticonvulsant activity. Farmaco 2004, 59 (11), 893-901.

27. Kucukguzel, S.; Rollas, S.; Erdeniz, H.; Kiraz, M.; Cevdet Ekinci, A.; Vidin, A. Synthesis, characterization and pharmacological properties of some 4-arylhydrazono-2-pyrazoline-5-one derivatives obtained from heterocyclic amines. European Journal of Medicinal Chemistry 2000, 35 (7-8), 761-771.

28. Kucukguzel, S.; Oruc, E. E.; Rollas, S.; Sahin, F.; Ozbek, A. Synthesis, characterisation and biological activity of novel 4-thiazolidinones, 1,3,4-oxadiazoles and some related compounds. Eur. J. Med. Chem. 2002, 37 (3), 197-206.

29. Kucukguzel, S.; Kocatepe, A.; De Clercq, E.; Sahin, F.; Gulluce, M. Synthesis and biological activity of 4-thiazolidinones, thiosemicarbazides derived from diflunisal hydrazide. Eur. J. Med. Chem 2006, 41 (3), 353-359.

30. Kucukguzel, S. G.; Rollas, S. Synthesis, characterization of novel coupling products and 4-arylhydrazono-2-pyrazoline-5-ones as potential antimycobacterial agents. Farmaco 2002, 57 (7), 583-587.

31. Kucukguzel, S. G.; Mazi, A.; Sahin, F.; Ozturk, S.; Stables, J. Synthesis and biological activities of diflunisal hydrazide-hydrazones. Eur. J. Med. Chem 2003, 38 (11-12), 1005-1013.

32. Maccari, R.; Ottana, R.; Monforte, F.; Vigorita, M. G. In vitro antimycobacterial activities of 2'-monosubstituted isonicotinohydrazides and their cyanoborane adducts. Antimicrob. Agents Chemother. 2002, 46 (2), 294-299.

33. Maccari, R.; Ottana, R.; Vigorita, M. G. In vitro advanced antimycobacterial screening of isoniazid-related hydrazones, hydrazides and cyanoboranes: part 14. Bioorg. Med. Chem. Lett. 2005, 15 (10), 2509-2513.

34. Monge, A.; Lopez de, C. A.; Montoya, M. E.; Ortega, M. A.  Investigación de nuevos agentes antituberculosos derivados de quinoxalinas. Report of CYTED's Coordination Meeting, 1997 Objetivos terapéuticos para el año 2000: una visión latinoamericana.  2007.

Ref Type: Abstract

35. Montoya, M. E.; Sainz, Y.; Ortega, M. A.; Lopez de, C. A.; Monge, A. Synthesis and antituberculosis activity of some new 2-quinoxalinecarbonitriles. Farmaco 1998, 53 (8-9), 570-573.

36. Montoya, M. E.; Sainz, Y.; Ortega, M. A.; Lopez de, C. A.; Monge, A.  Derivados de quinoxalina. Nuevos fármacos de potencial utilidad en el tratamiento de la tuberculosis.  Organización de farmacéuticos Iberolatinoamericanos (OFIL). 1998, 8 (3), 36-41.

37. Ortega, M. A.; Sainz, Y.; Montoya, M. E.; Lopez de, C. A.; Monge, A. Synthesis and antituberculosis activity of new 2-quinoxalinecarbonitrile 1,4-di-N-oxides. Pharmazie 1999, 54 (1), 24-25.

38. Ortega, M. A.; Montoya, M. E.; Jaso, A.; Zarranz, B.; Tirapu, I.; Aldana, I.; Monge, A. New quinoxaline derivatives showing antituberculosis activity.  Nuevas Técnicas de Screening en el Descubrimiento de Medicamentos (CYTED). 2000, 10.

39. Ortega, M. A.; Montoya, M. E.; Jaso, A.; Zarranz, B.; Tirapu, I.; Aldana, I.; Monge, A. Antimycobacterial activity of new quinoxaline-2-carbonitrile and quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Pharmazie 2001, 56 (3), 205-207.

40. Ortega, M. A.; Sainz, Y.; Montoya, M. E.; Jaso, A.; Zarranz, B.; Aldana, I.; Monge, A. Anti-Mycobacterium tuberculosis agents derived from quinoxaline-2-carbonitrile and quinoxaline-2-carbonitrile 1,4-di-N-oxide. Arzneimittelforschung. 2002, 52 (2), 113-119.

41. Sainz, Y.; Montoya, M. E.; Martinez-Crespo, F. J.; Ortega, M. A.; Lopez de, C. A.; Monge, A. New quinoxaline 1,4-di-N-oxides for treatment of tuberculosis. Arzneimittelforschung. 1999, 49 (1), 55-59.

42. Sainz, Y.; Martinez-Crespo, F. J.; Montoya, M. E.; Ortega, M. A.; Aldana, I.; Lopez de, C. A.; Monge, A. Synthesis and antituberculosis activity of new quinoxaline 1,4-di-N-oxides and 2-quinoxalinecarbonitriles. Methods and Findings. 1999, 21 (A), 129.

43. Savini, L.; Chiasserini, L.; Gaeta, A.; Pellerano, C. Synthesis and anti-tubercular evaluation of 4-quinolylhydrazones. Bioorg. Med. Chem. 2002, 10 (7), 2193-2198.

44. Seitz, L. E.; Suling, W. J.; Reynolds, R. C. Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives. J. Med. Chem. 2002, 45 (25), 5604-5606.

45. Suling, W. J.; Seitz, L. E.; Reynolds, R. C.; Barrow, W. W. New Mycobacterium avium antifolate shows synergistic effect when used in combination with dihydropteroate synthase inhibitors. Antimicrob. Agents Chemother. 2005, 49 (11), 4801-4803.

46. Ulusoy, N.; Capan, G.; Otuk, G.; Kiraz, M. Synthesis and antimicrobial activity of new 6-phenylimidazo[2,1-b]thiazole derivatives. Boll. Chim. Farm. 2000, 139 (4), 167-172.

47. Ulusoy, N.; Gursoy, A.; Otuk, G. Synthesis and antimicrobial activity of some 1,2,4-triazole-3-mercaptoacetic acid derivatives. Farmaco 2001, 56 (12), 947-952.

48. Ulusoy, N.; Ergenc, N.; Otuk, G.; Kiraz, M. Synthesis of some 4-(alkylidene/arylidene)amino-2,4-dihydro-5- (2-thienyl)-3H-1,2,4-triazole-3-thiones tested for antimicrobial activity. Boll. Chim. Farm. 2001, 140 (6), 417-421.

49. Ulusoy, N.; Kiraz, M.; Kucukguzel, G.  New 6-(4-bromophenyl_imidazo[2, 1-b]thiazole derivatives: Synthesis and antimicrobial activity. Monatsh. Chem. 2002.

50. Walczak, K.; Gondela, A.; Suwinski, J. Synthesis and anti-tuberculosis activity of N-aryl-C-nitroazoles. Eur. J. Med. Chem. 2004, 39 (10), 849-853.

51. Waring, M. J.; Ben-Hadda, R.; Kotchevar, A. T.; Ramdani, A.; Touzani, R.; Elkadiri, S.; Hakkou, A.; Bouakka, M.; Ellis, T. 2,3-bifunctionalized quinoxalines: Synthesis, DNA interactions and evaluation of anticancer, anti-tuberculosis and anti-fungal activity. Molecules 2002.

52. Zarranz, B.; Jaso, A.; Aldana, I.; Monge, A. Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives. Bioorg. Med. Chem 2003, 11 (10), 2149-2156.

Reviews and Summaries of TAACF Activities

  1. Goldman, R.; Laughon, B.; Franzblau, S.; Krahenbuhl, J.; Adams, A.; Lenaerts, A.; Orme, I.; Secrist, J.; Young, L.; Plumley, K.; Lambros, C.  New Agents for Drug Resistant Tuberculosis (TB). Conference on Antimicrobial Resistance, Hyatt Regency Bethesda. 2006.

Ref Type: Abstract

  2. Goldman, R. C.; Laughon, B. E.; Reynolds, R.; Secrist, J.; Maddry, J.; Guie, M.; Poffenberger, A.; Kwong, C.; Subramaniam, A. Programs to Facilitate Tuberculosis Drug Discovery: The Tuberculosis Antimicrobial Acquisition and Coordinating Facility. Infectious Disease - Drug Targets 2007.

  3. Laughon, B. E. New tuberculosis drugs in development. Curr. Top. Med Chem 2007, 7 (5), 463-473.

  4. Orme, I. Search for new drugs for treatment of tuberculosis. Antimicrob. Agents Chemother. 2001, 45 (7), 1943-1946.

  5. Plumley, K.; Laughon, B. E.; Goldman, R. C.; Secrist, J.; Franzblau, S.; Krahenbuhl, J.; Rouse, D.; Lenaerts, A. J.; Orme, I.  TAACF: Tuberculosis Antimicrobial Acquisition and Coordinating Facility.  6-16-2006. Lisbon, Portugal; 12th International Congress on Infectious Disease.

Ref Type: Audiovisual Material

  6. Zhang, Y. The magic bullets and tuberculosis drug targets. Annu. Rev Pharmacol. Toxicol. 2005, 45, 529-564.

Compounds with In Vitro Data

 

    1. Al-Saadi, M. S. M., Rostom, S. A. F., Sheriff, A. F., and Faidallah, H. M. M.  Synthesis and microbiological evaluation of novel 3-cyano-4-(1-methyl-1H-pyrrol-2-yl)-6-substituted-2(1H)-pyridinones and their 2-imino bioisosters. Alexandria Journal of Pharmaceutical Sciences 2005, 19 (1), 15-21.

    2. Alahari, A., Trivelli, X., Guerardel, Y., Dover, L. G., and Besra, G. S.  Thiacetazone, an Antitubercular Drug that Inhibits Cyclopropanation of Cell Wall Mycolic Acids in Mycobacteria.  PLoS ONE 2007, 2 (12).

    3. Alksnis, E., Kornejeva, D., and Lukevics, E.  Derivatives of adenine and uracil with antituberculosis activity. HIMIA GETEROCIKLICHESKIH SOEDINENIJ (Chemistry of Heterocyclic Compounds (Riga, Latvia) 2001, 6 807-810.

    4. Anaflous, A., Benchat, N., Mimouni, S., Abouricha, S., Ben-Hadda, T., El-Bali, A., and Hacht, B.  Armed Imidazo [1,2-a] Pyrimidines (Pyridines): Evaluation of Antibacterial Activity. Lett.Drug Des.& Disc 2004, 1 35-44.

    5. Andresen, G., Gundersen, L. L., Nissen-Meyer, J., Rise, F., and Spilsberg, B.  Cytotoxic and antibacterial activity of 2-oxopurine derivatives. Bioorg.Med Chem Lett. 2002, 12 (4), 567-569.

    6. Bakkestuen, A. K., Gundersen, L. L., Langli, G., Liu, F., and Nolsoe, J. M.  9-Benzylpurines with inhibitory activity against Mycobacterium tuberculosis. Bioorg.Med Chem Lett. 2000, 10 (11), 1207-1210.

    7. Bakkestuen, A. K., Gundersen, L. L., and Utenova, B. T.  Synthesis, biological activity, and SAR of antimycobacterial 9-aryl-, 9-arylsulfonyl-, and 9-benzyl-6-(2-furyl)purines. J.Med Chem 2005, 48 (7), 2710-2723.

    8. Bakkestuen, A. K., Gundersen, L. L., Peterson, P., Utenova, B. T., and Vik, A.  Synthesis and Antimycobacterial Activity of Agelasine E and Analogs. Org.Biol.Chem. 2005, 3 1025-1033.

    9. Baumgartner, J. and Weber, H.  From 6-t-butylfulvene to highly functionalized five-membered rings. Chirality 2001, 13 (3), 159-163.

  10. Ben-Hadda, T., Kotchevar, A. T., Daoudi, M., Bennani, B., Ben Larbi, N., and Kerbal, A.  Anti-tumour Activity of Some Polydentate N-Ligands: N,N-bis-(3-Substituted-5-Methylpyrazol-1yl Methyl) Arylamines and N,N,N',N'-Tetra-[(3-Substituted-5-Methylpyrazol-1yl] Para-Phenylenediamines. Letters in Drug Design & Discovery. 2005, 2 584-589.

  11. Benhaliliba, H., Derdour, A., Bazureau, J. P., Texier-Boullet, F., and Hamelin, J.  Solvent free oxidation of [beta], [beta]-disubstituted enamines under microwave irradiation. Tetrahedron Letters 1998, 39 (7), 541-542.

  12. Bennani, B., Kerbal, A., Ben Larbi, N., and Ben-Hadda, T.  Synthesis and application of spir-isoxazolines as new anti-tubercular agents.2004, (Moroccan Patent No. 2769).

  13. Bennani, B., Kerbal, A., Ben Larbi, N., and Ben-Hadda, T.  Synthesis and application of some sprio-isoxazolines as new anti-HIV agents.2004, (Moroccan Patent No. 2770).

  14. Bennani, B., Kerbal, A., Ben Larbi, N., and Ben-Hadda, T.  Synthesis and application of des iso-thio-chromeno[3,4-e][1,2]oxazine (TCO) as new anti-tumoral agents.2004, (Moroccan Patent 2771).

  15. Berree, F., Bazureau, J. P., Michelot, G., and Le Corre, M.  N-Boc and N-Cbz ethyl oxamates: New Gabriel reagents. Synthetic Communications 1999, 29 (15), 2685-2693.

  16. Bhatt, A. H. and Parekh, H.  Synthesis of pyrazoles and isoxazoles as potential antimicrobial agents. Heterocyclic Communications. 1998, 4 (4).

  17. Bhatt, A. H., Parekh, H., and Parikh, A. R.  Synthesis and biological screening of some novel sulphonamides and aryl sulphonates. J.Inst.Chem. 1999, 71 (21).

  18. Bottari, B., Maccari, R., Monforte, F., Ottana, R., Rotondo, E., and Vigorita, M. G.  Isoniazid-related copper(II) and nickel(II) complexes with antimycobacterial in vitro activity. Part 9. Bioorg.Med Chem Lett. 2000, 10 (7), 657-660.

  19. Braendvang, M. and Gundersen, L. L.  Selective anti-tubercular purines: synthesis and chemotherapeutic properties of 6-aryl- and 6-heteroaryl-9-benzylpurines. Bioorg.Med Chem 2005, 13 (23), 6360-6373.

  20. Braendvang, M. and Gundersen, L. L.  Synthesis, Biological Activity and SAR of Antimycobacterial 2- and 8-Substituted 6-(2-Furyl)-9-(p-methoxybenzyl)purines. Bioorg.Med Chem 2007, 15 7144-7165.

  21. Brugidou, R., Dahmani, Z., Rahmouni, M., Bazureau, J. P., and Hamelin, J.  Stereoselective synthesis of (2E) 3-amino-2-(1H-benzimidazol-2-yl) acrylate and symmetric bis-acrylates by transamination reactions. Heteroatom Chem. 1999, 10 (6), 446-454.

  22. Bukowski, L.  Some reactions of 2-cyanomethyl-3-methyl-3H-imidazo[4,5-b]pyridine with isothiocyanates. Antituberculotic activity of the obtained compounds. Pharmazie 2001, 56 (1), 23-27.

  23. Businelli, S., Di Martino, E., and Zanirato, P.  New insight on the cycloaddition of aryl and heteroaryl azides with (trimethlsilyl)acetylene. Spectroscopic and X-ray crystallographic data of silyated 1,2,3-triazoles. Arkivoc, Arkat USA. 2001,  2 (1), 131.

  24. Cado, F., Bazureau, J. P., and Hamelin, J.  Synthesis of 2-oxo-D2-pyrrolino-[1,2-alpha]-(4H)-permidine by N, C-cyclocondensation to a heterocyclic ketene aminal. Bulletin Societe Chimique 1996, 105 (5), 273-278.

  25. Cado, F., Di-Martino, J. L., Jacquault, P., Bazureau, J. P., and Hamelin, J.  Amidine-enediamine tautomerism: addition reaction of isocyanates to 2-substituted (1H)-perimidines. Some synthesis under microwave irradiation. Bulletin Societe Chimique 1996, 133.

  26. Cado, F., Dozias, J., Jacquault, P., Bazureau, J. P., and Hamelin, J.  Tandem conjugate C-addition/intermolecular hetero Diels-Alder reactions using perimidine as ketene-aminal under microwaves. J.Chem.Res.(S) 1997, 176-177.

  27. Cado, F., Bazureau, J. P., and Hamelin, J.  Regioselective aza-annulation to a heterocyclic keten aminal: A new route to ethyl-1-oxo-2, 3-dihydropyrido-[1, 2-a]-(5H)-perimidine-4-carboxylate. Heteroatom Chemistry 1998, 9 (5), 523-528.

  28. Carta, A., Sanna, P., Palomba, M., Vargiu, L., La, C. M., and Loddo, R.  Synthesis and antiproliferative activity of 3-aryl-2-(1H-benzotriazol-1-yl)acrylonitriles. Part III. Eur.J.Med Chem 2002, 37 (11), 891-900.

  29. Cherouvrier, J. R., Boissel, J., Carreaux, F., and Bazureau, J. P.  A Stereoselective Route to 3-Methyl-2-methylsulfanyl-5-yliden-3, 4-dihydro-imidazol-4-one Derivatives and Precursor of Leucettamine B.  Green Chemistry 2001, 3 165-169.

  30. Cherouvrier, J. R., Carreaux, F., and Bazureau, J. P.  Microwave mediated solventless synthesis of new derivatives of Marine Alkaloid Leucettamine B.  Tetrahedron Lett. 2002, 43 3581-3584.

  31. Chlupacova, M., Opetalova, V., Kunes, J., Silva, L., Buchta, V., Duskova, L., and Kralova, K.  Synthesis and Biological Evaluation of Some Ring-substituted (E)-3-Aryl-1-pyrazin-2-ylprop-2-en-1-ones.   Folia Pharm.Univ.Carol. 2005,  33 31-43.

  32. Cociorva, O. M., Gurcha, S. S., Besra, G. S., and Lowary, T. L.  Oligosaccharides as inhibitors of mycobacterial arabinosyltransferases. Di- and trisaccharides containing C-3 modified arabinofuranosyl residues. Bioorg.Med Chem 2005, 13 (4), 1369-1379.

  33. Constantine, G. H., Karchesy, J. J., Franzblau, S. G., and LaFleur, L. E.  (+)-Totarol from Chamaecyparis nootkatensis and activity against Mycobacterium tuberculosis. Fitoterapia 2001, 72 (5), 572-574.

  34. Copp, B. R., Christiansen, H. C., Lindsay, B. S., and Franzblau, G.  Identification of heteroarylenamines as a new class of antituberculosis lead molecules. Bioorg.Med Chem Lett. 2005, 15 (18), 4097-4099.

  35. Dahmani, Z., Rahmouni, M., Brugidou, R., Bazureau, J. P., and Hamelin, J.  A new route to [alpha]-hetero [beta]-enamino esters using a mild and convenient solvent-free process assisted by focused microwave irradiation. Tetrahedron Letters 1998, 39 (46), 8453-8456.

  36. Desai, B., Sureja, D., Naliapara, Y., Shah, A., and Saxena, A. K.  Synthesis and QSAR studies of 4-substituted phenyl-2,6-dimethyl-3, 5-bis-N-(substituted phenyl)carbamoyl-1,4-dihydropyridines as potential antitubercular agents. Bioorg.Med Chem 2001, 9 (8), 1993-1998.

  37. Dolezal, M., Hartl, J., and Miletin, M.  Antimycobacterial evaluation of some anilides of pyrazine-2-carboxylic acid. Folia Pharm.Univ.Carol 2000, 25 15-19.

  38. Dolezal, M., Vicik, R., Miletin, M., and Kralova, K.  Synthesis and antimycobacterial, antifungal, and photosynthesis-inhibiting evaluation of some anilides of substituted pyrazine-2-carboxylic acids. Chem.Papers 2000, 54 245-248.

  39. Dolezal, M., Cmedlova, P., Palek, L., Vinsova, J., Kunes, J., Buchta, V., Jampilek, J., and Kralova, K.  Synthesis and antimycobacterial evaluation of substituted pyrazinecarboxamides. Eur.J.Med Chem 2007, Article in press.

  40. Doshi, R., Kagthara, P., and Parekh, H.  Synthesis and biological evaluation of some novel isoxazoles and cyanopyridines a new class of potential anti-tubercular agents. Indian J.Chem 1999, 38B 348-352.

  41. Dubreuil, J. F. and Bazureau, J. P.  Rate accelerations of 1,3-dipolar cycloaddition reactions in ionic liquids. Tetrahedron Letters 2000, 41 (38), 7351-7355.

  42. El Sayed, K. A., Bartyzel, P., Shen, X., Perry, T. L., Zjawiony, J. K., and Hamann, M. T.  Marine Natural Products as Antituberculosis Agents. Tetrahedron 2000, 56 (7), 949-953.

  43. El Sayed, K. A., Kelly, M., Kara, U. A., Ang, K. K., Katsuyama, I., Dunbar, D. C., Khan, A. A., and Hamann, M. T.  New manzamine alkaloids with potent activity against infectious diseases. J.Am.Chem Soc. 2001, 123 (9), 1804-1808.

  44. Ferrarini, P. L., Manera, C., Mori, C., Badawneh, M., and Saccomanni, G.  Synthesis and evaluation of antimycobacterial activity of 4-phenyl-1,8-naphthyridine derivatives. Farmaco 1998, 53 (12), 741-746.

  45. Fraga-Dubreuil, J., Cherouvrier, J., and Bazureau, J. P.  Clean solvent free dipolar cycloaddtion assisted by focused microwave irradiataion for a new synthesis of ethyl-4-cyano-2-oxazoline-4-carboxylate. Green Chemistry 2000, 4 226-229.

  46. Fraga-Dubreuil, J. and Bazureau, J. P.  Grafted ionic liquid-phase-supported synthesis of small organic molecules. Tetrahedron Letters 2001, 42 (35), 6097-6100.

  47. Fraga-Dubreuil, J., Famelart, M., and Bazureau, J. P.  Ecofriendly fast synthesis of hydrophilic poly(ethyleneglycol)-ionic liquid matrix for liquid phase organic synthesis. Org.Process.& Res.Dev. 2002, 42 374-378.

  48. Fraga-Dubreuil, J., Bourahla, K., Rahmouni, M., Bazureau, J. P., and Hamelin, J.  Catalysed esterifications in room temperature ionic liquids with acidic counteranion as recyclable reaction media. Catalysis Communications 2002, 3 (5), 185-190.

  49. Gondela, A. and Walczak, K.  A convenient method for N-1 arylation of uracil derivatives. Tetrahedron Letters 2006, 47 (27), 4653-4657.

  50. Gondela, A., Sroka, M., and Walczak, K.  1-(2,4-Dinitrophenyl)-5-nitrouracil a Versatile Reagent for the Synthesis of N1-Modified

Uracil Derivatives. Polish J.Chem. 2007, 81 2143-2149.

  51. Gundersen, L. L., Nissen-Meyer, J., and Spilsberg, B.  Synthesis and antimycobacterial activity of 6-arylpurines: the requirements for the N-9 substituent in active antimycobacterial purines. J.Med Chem 2002, 45 (6), 1383-1386.

  52. Gundersen, L. L., Negussie, A. H., Rise, F., and Østby, O. B.  Antimycobacterial Activity of 1-Substituted Indolizines.  Arch.Pharm.Pharm.Med.Chem. 2003, 336 191-195.

  53. Gundersen, L. L., Charnock, C., Negussie, A. H., Rise, F., and Teklu, S.  Synthesis of indolizine derivatives with selective antibacterial activity against Mycobacterium tuberculosis. Eur.J.Pharm.Sci. 2007, 30 (1), 26-35.

  54. Hearn, M. J. and Cynamon, M. H.  Design and synthesis of antituberculars: preparation and evaluation against Mycobacterium tuberculosis of an isoniazid Schiff base. J.Antimicrob.Chemother. 2004, 53 (2), 185-191.

  55. Heinisch, G., Matuszczak, B., and Planitzer, K.  Pyridazines 91. Synthesis of substituted tri- and tetracyclic compounds bearing a pyridazine core and their biological evaluation as antimycobacterial agents. Arch.Pharm.(Weinheim) 2000, 333 (7), 231-240.

  56. Himdi-Kabbab, S., Lavrador, K., Bazureau, J. P., and Hamelin, J.  Synthesis of 1, 4, 5, 6-Tetrahydro 2-Methyl 4-Pyrimidine Carboxylic Acid: Osmoprotector Amino Acid.Taylor & Francis.  Synthetic Communications 1995, 25 (15), 2223-2227.

  57. Hu, J. and Miller, M. J.  Total Synthesis of a Mycobactin S, a Siderophore and Growth Promoter of Mycobacterium Smegmatis, and Determination of its Growth Inhibitory Activity against Mycobacterium tuberculosis. Journal of the American Chemical Society 1997, 119 (15), 3462-3468.

  58. Hu, J. F., Schetz, J. A., Kelly, M., Peng, J. N., Ang, K. K., Flotow, H., Leong, C. Y., Ng, S. B., Buss, A. D., Wilkins, S. P., and Hamann, M. T.  New antiinfective and human 5-HT2 receptor binding natural and semisynthetic compounds from the Jamaican sponge Smenospongia aurea. J.Nat Prod. 2002, 65 (4), 476-480.

  59. Ishikawa, T.  Benzo[c]phenanthridine bases and their antituberculosis activity. Med Res.Rev 2001, 21 (1), 61-72.

  60. Ivanov, I. C., Stoyanov, V., Denkova, P. S., and Dimitrov, V. S.  Synthesis of Substituted 1,2-Dihydro-2-imino-7-methyl-1,6(6H)-naphthyridin-5-ones. Liebigs.Ann./ Recueil 1997, 1977-1981.

  61. Jampilek, J., Dolezal, M., and Buchta, V.  Antimicrobial evaluation of some arylsulfanylpyrazinecarboxylic acid derivatives.Bentham Science Publishers.  Medicinal Chemistry 2007, 3 (3), 277-280.

  62. Joshi, D. G., Oza, H. B., and Parekh, H.  Synthesis of some novel 1, 3, 4- Oxadiazoles and 5- oxo- inidazolines as potent biologically active agents. Heterocyclic Communication. 1997, 3 (2), 169-174.

  63. Jouneau, S. and Bazureau, J. P.  Solvent free aza-annulation using 4-dimethylamino 2-aza-1,3-dienes as [gamma]-dielectrophiles for a new synthesis of imidazole-4-carboxylates. Tetrahedron Letters 1999, 40 (46), 8097-8098.

  64. Kagthara, P., Shah, R., Doshi, R., and Parekh, H.  Synthesis of some Aryl amides, Sulphonamides and 5-Oxo imidazolines as novel bioactive compounds derived from benzimidazole. Heterocyclic Communication 1998, 4 (6),

  65. Kagthara, P., Shah, N., Doshi, R., and Parekh, H.  Synthesis of 2,5- disubstituted 1,3,4-oxadiazoles as biologically active heterocycles. 1.Indian J.Chem.1999, 38(B): 572-576.  1999, 38b 572-576.

  66. Kagthara, P., Upadhyay, T., Doshi, R., and Parekh, H.  Synthesis of some 2-azetidione as potiental antitubercular agents. Indian J.Heterocyclic Chem 2000, 10 (9).

  67. Karali, N., Terzioolu, N., and Gursoy, A.  Synthesis and structure-activity relationships of 3-hydrazono-1H-2-indolinones with antituberculosis activity. Arzneim.Forsch./Drug Res. 1998, (48), 758-763.

  68. Kerneur, G., Lerestif, J. M., Bazureau, J. P., and Hamelin, J.  Convenient preparation of 4-alkylidene-1H-imidazol-5-(4H)-one derivatives using imidate and aldehydes by solvent-free cycloaddition under microwaves. Synthesis 1997, 3 287-289.

  69. Kiec-Kononowicz, K., Szymanska, E., Motyl, M., Holzer, W., Bialecka, A., and Kasprowicz, A.  Synthesis, spectral and antimicrobial properties of 5-chloroarylidene aromatic derivatives of imidazoline-4-one. Pharmazie 1998, 53 (10), 680-684.

  70. Kobarfard, F., Kaufmann, J., and Joel, M.  Synthesis of fluorinated analogs of antitubercular drugs. Book of Abstracts 2000.

  71. Kucukguzel, S. G., Rollas, S., Kucukguzel, I., and Kiraz, M.  Synthesis and antimycobacterial activity of some coupling products from 4-aminobenzoic acid hydrazones. European Journal of Medicinal Chemistry 1999, 34 (12), 1093-1100.

  72. Laddi, U. V., Talawar, M. B., Desai, S. R., Bennur, R. S., and Bennur, S. C.  Synthesis, antimicrobial and antituberculosis activities of N-bridged heterocycles. Indian Journal of Chemistry 2001, 40B 823-833.

  73. Lerestif, J. M., Bazureau, J. P., and Hamelin, J.  Cycloaddition with stabilized imidates as potential azomethines ylides : A new route to 2-imidazoline and 4-yliden-s-imidazolinone. Tetrahedron Letters 1993, 34 (29), 4639-4642.

  74. Lerestif, J. M., Bazureau, J. P., and Hamelin, J.  Efficient and Practical New Synthesis of 2-Oxazolines; 1,2-Bis- and 1,3-Bis(oxazolinyl)benzenes by [3+2] Cycloaddition Using Solvent-Free Conditions. Synlett 1995, (06), 647-649.

  75. Lerestif, J. M., Bazureau, J. P., and Hamelin, J.  1, 3-Dipolar cycloaddition of imidate ylides on imino-alcohols: synthesis of new imidazolones using solvent free conditions. Tetrahedron Letters 1995, 51 6757-6774.

  76. Lerestif, J. M., Toupet, L., Sinbandhit, S., Tonnard, F., Bazureau, J. P., and Hamelin, J.  A new route to 2-oxazolines, bis-oxazolines, and 2-imidazoline-5-ones from imidates using solvent-free cycloadditions: Synthesis, chemical properties, and PM3 MO calculations. Tetrahedron 1997, 53 (18), 6351-6364.

  77. Lerestif, J. M., Feuillet, S., Bazaureau, J. P., and Hamelin, J.  Novel synthesis of protected methyl 4-hydroxy-1, 2, 3, 4-tetrahydroisoquinolin-3-carboxylate via cleavage of functionalized oxazoline. J.Chem.Res. 1999, Supplement 32-33.

  78. Lin, Y. M., Flavin, M. T., Cassidy, C. S., Mar, A., and Chen, F. C.  Biflavonoids as novel antituberculosis agents. Bioorg.Med Chem Lett. 2001, 11 (16), 2101-2104.

  79. Lin, Y. M., Zhou, Y., Flavin, M. T., Zhou, L. M., Nie, W., and Chen, F. C.  Chalcones and flavonoids as anti-tuberculosis agents. Bioorg.Med Chem 2002, 10 (8), 2795-2802.

  80. Macaev, F., Rusu, G., Pogrebnoi, S., Gudima, A., Stingaci, E., Vlad, L., Shvets, N., Kandemirli, F., Dimoglo, A., and Reynolds, R.  Synthesis of novel 5-aryl-2-thio-1,3,4-oxadiazoles and the study of their structure-anti-mycobacterial activities. Bioorg.Med Chem 2005, 13 (16), 4842-4850.

  81. Maddry, J. A., Suling, W. J., and Reynolds, R. C.  Glycosyltransferases as targets for inhibition of cell wall synthesis in M. tuberculosis and M. avium. Res.Microbiol. 1996, 147 (1-2), 106-112.

  82. Maddry, J. A., Bansal, N., Bermudez, L. E., Comber, R. N., Orme, I. M., Suling, W. J., Wilson, L. N., and Reynolds, R. C.  Homologated aza analogs of arabinose as antimycobacterial agents. Bioorg.Med Chem Lett. 1998, 8 (3), 237-242.

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