Keywords
Mycobacterium tuberculosis
Antimycobacterial activity
Susceptibility test
Alamar Blue
Antimycobacterial activity
Susceptibility test
Alamar Blue
How to Cite
1.
Nakamura Sato D, Terezinha M. Bacha C, Garibotti D, Bottcher M, Clarice Errera M, Presotto P, Elias Andrade Melles C. Minimal inhibitor concentration and minimal bactericidal concentration determination of isonicotinic acid derivatives against Mycobacterium tuberculosis. Rev Inst Adolfo Lutz [Internet]. 1999 Jun. 30 [cited 2024 May 18];58(1):25-31. Available from: https://periodicos.saude.sp.gov.br/RIAL/article/view/36655
Abstract
Tuberculosis still remains as a worldwide Public Health problem with high morbidity and mortality in developing countries. The increase of strains of Mycobacterium tuberculosis that are resistant to antimycobacterial agents is a worldwide problem. Consequently, it is urgently necessary to develop antimycobacterial drugs which are more effective than those used in conventional treatment of tuberculosis. Twelve isonicotinic acid derivatives were evaluated for in vitro activity against Mycobacterium tuberculosis H37Ra ATCC 25177. The MIC and Minimal Bactericidal Concentration (MBC) of Mycobacterium tuberculosis H37Ra was determined by broth macrodilution method. The Minimal Inhibitory Concentration (MIC) of all derivatives showed a range of 0,062 to 0,250 ug/ml.. In general, the MBC values for all derivatives were two-fold higher than their corresponding MICs values. These MICs and MBCs values are close to isoniazid, that was considered the gold standard in this study.
References
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25. KIM, S.1.; BAI, G.H. and HONG, Y.P. Drug-resistant tuberculosis in Korea, 1994. Int. J. Tuberc. Lung Dis., 1: 302-8,1997.
26. KOCHI, A.; VARELDZIS, B.; STYBLO, K. Mu1tidrug-resistant tuberculosis and its controI. Rev. MicrobioI., 144: 104-10, 1993.
27. McMACKEN, M. Y CASTRO, K.G. La tuberculosis y el virus de Ia inmunodeficiencia humana en los Estados Unidos, 1985-1992, BoI. Oficina Sanit. Panam., 117: 77-83,1994.
28. MELO, F.A.F. e AFIUNE, J.B. Quimioterapia da tuberculose: bases, condutas e procedimentos. J. Pneurnol., 19: 42-9,1993
29. MUSSER, J.M. Antimicrobial agent resistance in mycobacteria: molecular genetic insights. C1in. MicrobioI. Rev., 8: 496-514, 1995.
30. RAVIGLIONE, M.C; DYE, e; SCHMIDT, S.; KOCHI, A. & The WHO Global Surveillance and Monitoring Project. Assessment of worldwide tuberculosis controI. Lancet, 350: 624-9, 1997.
31. SALEM, J.I.; GOH, K.S.; LITAIFF, L.RL.; CARCLOSO, M.S.L. e BRIGLIA, M.F.S. An investigation of primary and acquired drug resistence of Mycobacterium tuberculosis in Manaus (Amazonas, Brazil). J. Pneumol., 16: 6-8,1990.
32. SIDDIQI, S.H.; HEIFETS, L.B.; CYNAMON, M.H.; HOOPER, N.M.; LAZLO, A.; LIBONATI, J.P.; LINDHOLM-LEVY, P.J. & PEARSON,N. Rapid broth macrodilution method for determination of MICs for Mycobacterium avium isolates. J. Clin. Microbiol., 31: 2332-8, 1993.
33. SILVA, E.A.M.; SATO, D.N.; TELLES, M.A.S.; MARTINS, M.e; PALACI, M. e UEKI, S.Y.M. Perfil de Resistência de Mycobacterium tuberculosis no Estado de São Paulo, 1986 a 1990. Rev. Inst. Adolfo Lutz, 52: 37-40, 1992.
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36. TOMAN, K. Tuberculosis: case-finding and chemotherapy. Questions and answers. World Health Organization, 1979.
37. TSUKAMURA, M. In vitro bacteriostatic and bactericidal activity of isoniazid on the
Mycobacterium avium-Mycobacterium intracellulare complexo Tubercle, 71:199-204,1990.
38. VIGORITA, M.G.; BASILE, M.; ZAPPALÀ, e; GABRIELLI, G. and PIZZIMENTI, F.
Halogenated isoniazid derivatives as possible antitubercular and antineoplastic agents. Note 1. 11Farmaco, 47: 893-903, 1992.
39. VISKUM, K. and JOK-JENSEN,A. Multidrug-resistant tuberculosis in Denmark 1993-1995. Int. J. Tuberc. Lung. Dis., 1: 299-301., 1997.
40. VOYATZAKIS, VA.E.; VASlLIKIOTIS, G.S.; KARAGEORGIOU, G. & KASSAPOGLOU, I.R lnfluence of metallic ions on the antituberculous activity of isonicotinoyl hydrazones. J. Pharm. Sci., 57: 1255-7, 1968.
41. WORLD HEALTH ORGANIZATION. WHO Report on the Tuberculosis Epidemic. Tuberculosis (TB) Annual Report - DOTS (Directly Observed Treatment, Short-course) A Breakthrough in TB Control, 40 p., 1997.
42. YAMAMOTO, S.; TOIDA, 1.; WATANABE, N. and URA, T. In vitro antimycobacterial activities of pyrazinamide analogs. Antimicrob. Agents Chemother., 39: 2088-91, 1995.
43. YEW, W.W. and CHAU, CH. Drug-resistant tuberculosis in the 1990s. Eur. Resp. J., 8: 1184-92, 1995.
44. YOUNG, D.B. Strategies for new drug development. ln: Bloom, B.R (ed.) Tuberculosis: Pathogenesis, Protection and Control. American Society for Microbiology, Washington, D.e, 1ST Ed., 1994, p. 559-567.
2. BACHA, C.T.M.; SCHAPOVAL, E.E.S.; BOTTCHER, M.; GARAKE, J.E.; PRESOTTO, P. e GARIBOTTI, D.P. Síntese de novos compostos com potencial atividade antibacteriana e antifúngica derivados do ácido nicotínico. In: 49 a REUNIÃO ANUAL DA SOCIEDADE BRASILEIRA PARA O PROGRESSO DA CIÊNCIA, Belo Horizonte, 1997. Programas e Resumos. Belo Horizonte, Sociedade Brasileira para o Progresso da Ciência, 1997b.
3. BARRETO, A.M.W. e MARTINS, F.M. Estudo da resistência primária no Brasil no período de 1986 a 1988. Bol. Campanha Nac. Contra a Tuberc., 2: 21-5, 1988.
4. BEZEM, L.S.; VIEIRA, L.M.T.; ABRAHÃO, 1.S.; GOMES, C. e ANDRADE, A.l.S. Resistência primária aos tuberculostáticos no Estado de Santa Catarina. BoI. Campanha Nac. Contra a Tuberc., 2: 34-44, 1988.
5. BLOCH, A.B.; CAUTHEN, G.M.; ONORATO, LM.; DANSBURY, K.G.; KELLY, G.D.; DRIVER, C.R and SNIDER Ir, D.E. Nationwide survey of drug-resistant tuberculosis in the United States. lAMA, 271: 665-7l, 1994.
6. BRADFORD,W.Z.; MARTIN,l.N.; REINGOLD, A.L; SCHECTER, G.F.; HOPEWELL, PC. and SMALL,P.M. The changing epidemiology acquired drug-resistant tuberculosis in San Francisco, USA, Tubercle, 348: 928-31, 1996.
7. BRASIL. MINISTÉRIO DA SAÚDE. Centro Nacional de Epidemiologia. Coordenação de Pneumologia Sanitária. Manual de Normas para o controle da tuberculose. Série A: Normas e Manuais Técnicos, 13, Brasília, 1995.
8. BURMAN, W.J. The value of in vitro drug activity and pharmacokinetics in predicting the effectiveness of antimycobacterial therapy: a critica1 review. Am. J. Med. Sci., 313: 355-63, 1997.
9. CANTWELL, M.F.; SNIDER JR, D.E.; CAUTHEN, G.M. and ONORATO, T.M. Epidemiology of Tuberculosis in the United States, 1985 through 1992. lAMA, 272: 535-9, 1994.
10. CARPELS, G.; FISSETTE,K.; LIMBANA, V. VAN DEUN, A.; VANDENBULCKE,W., PORTAELS, F. Drug resistant tuberculosis in sub-Saharan Africa: an estimation of incidence and cost for the year 2000. Tuber. Lung. Dis., 76: 480-6, 1995.
11. CHAKRAVARTY, D.; BOSE, A. and BOSE, S. Synthesis and antitubercular activity of isonicotinoyl and cyanoacetyl hydrazones. 1. Pharmac. Sci., 53: 1036-9, 1963.
12. COHN, D.L.; BUSTREO, F. and RAVIGLIONE, M.C. Drug-Resistant Tuberculosis: Review of de Worldwide Situation and the WHO/ IUATLD Global Surveillance Project. Clin. Infec. Dis. 24( suppll): SI21-30, 1997.
13. DROBNIEWSKI, F.; TAYLER, E.; IGNATENKO, N.; PAUL, 1.L NYE, P.; LYAGOSHINA, T. and BESSE, C. Tuberculosis in Siberia: 1. An epidemiological and microbiological assessment. Tuber. Lung Dis., 77: 199-206, 1996.
14. ELBAGHDADI, 1.; LAZRAQ, R; IBRAHIMY, S.; BOUAYAD, Z.; GUINET, R and BENSLIMANE, A. Survey of primary drug resistance of Mycobacterium tuberculosis in Casablanca, Morocco. Int. 1. Tuberc. Lung Dis., I: 309-13, 1997.
15. ERICSSON, H.M. and SHERIS, 1.C. Antibiotic sensitivity testing: report for an international collaborative study. Acta Pathol. MicrobioI. Scand, [B] Supp1217: 3-90, 1971.
16. FRIEDEN, T.R; SHERMAN, L.F.; MAX, K.L.; FUJIWARA, P.I.; CRAWFORD, 1.T.; NIVIN ,B.; SHARP, v. HEWLETT Ir, D.; BRUDNEY, K.; ALLAND, D. and KREISWORTH,
B.N. A multi-institutional outbreak of highly drug-resistant tuberculosis: epidemiology and clinical outcomes. lAMA, 276: 1229-35,1996.
17. GARCIA, M.L.G.; GÓMEZ, 1.L.V.; SANCHO, M.C.G.; ÁLVAREZ, RA.S.; ZACARIAS, F. Y AMOR, 1.S. Epidemiologia dei SIDA y Ia tuberculosis. BoI. Oficina Sanit. Panam, 116: 546-64, 1994.
18. GERHARDT FO.,G. e HIJIAR,M.A. Aspectos epidemiológicos da tuberculose no Brasil. 1. PneumoI., 19: 4-10, 1993.
19. GRASSI, C. and PEONA, V. New drug for tuberculosis. Eur. Resp. 1., Suppl. 20P: 714s-8s, 1995. 20. GRUPO DE ESTUDIO DE TUBERCULOSIS RESISTENTE DE MADRID, Estudio transversal multihospitalario de tuberculosis y resistencias en Madrid (Octubre de 1993-Abril de 1994), Med. Clin.(Barc), 106: 1-6, 1996.
21. HAWKINS, J.E.; WALACE Jr, RJ. and BROWN, B.A. Antibacterial susceptibility test: Mycobacteria. In: Balows.A, (ed.) Manual of Clinical Microbiology. Washington D.C., 5th Ed., 1991, p. 1138-1152.
22. HEIFETS, L. Qualitative and quantitative drug-susceptibility tests in Mycobacteriology. Am. Rev. Resp. Dis., 137: 1217-22, 1988.
23. HOFFNER, S.E. Drug-resistant Mycobacterium tuberculosis; some data from Sweden, Estonia na Ethiopia. Scand. J. Infect. Dis. Suppl., 98: 17-8, 1995.
24. HOK, T.T. A comparative study of the susceptibillity to ethionamide, thiosemicarbazone, and isoniazid of tubercle bacilli from patients never treated with ethionamide or thiosemicarbazone. Am. Rev. Resp. Dis'l 90; 468-9l 1964.
25. KIM, S.1.; BAI, G.H. and HONG, Y.P. Drug-resistant tuberculosis in Korea, 1994. Int. J. Tuberc. Lung Dis., 1: 302-8,1997.
26. KOCHI, A.; VARELDZIS, B.; STYBLO, K. Mu1tidrug-resistant tuberculosis and its controI. Rev. MicrobioI., 144: 104-10, 1993.
27. McMACKEN, M. Y CASTRO, K.G. La tuberculosis y el virus de Ia inmunodeficiencia humana en los Estados Unidos, 1985-1992, BoI. Oficina Sanit. Panam., 117: 77-83,1994.
28. MELO, F.A.F. e AFIUNE, J.B. Quimioterapia da tuberculose: bases, condutas e procedimentos. J. Pneurnol., 19: 42-9,1993
29. MUSSER, J.M. Antimicrobial agent resistance in mycobacteria: molecular genetic insights. C1in. MicrobioI. Rev., 8: 496-514, 1995.
30. RAVIGLIONE, M.C; DYE, e; SCHMIDT, S.; KOCHI, A. & The WHO Global Surveillance and Monitoring Project. Assessment of worldwide tuberculosis controI. Lancet, 350: 624-9, 1997.
31. SALEM, J.I.; GOH, K.S.; LITAIFF, L.RL.; CARCLOSO, M.S.L. e BRIGLIA, M.F.S. An investigation of primary and acquired drug resistence of Mycobacterium tuberculosis in Manaus (Amazonas, Brazil). J. Pneumol., 16: 6-8,1990.
32. SIDDIQI, S.H.; HEIFETS, L.B.; CYNAMON, M.H.; HOOPER, N.M.; LAZLO, A.; LIBONATI, J.P.; LINDHOLM-LEVY, P.J. & PEARSON,N. Rapid broth macrodilution method for determination of MICs for Mycobacterium avium isolates. J. Clin. Microbiol., 31: 2332-8, 1993.
33. SILVA, E.A.M.; SATO, D.N.; TELLES, M.A.S.; MARTINS, M.e; PALACI, M. e UEKI, S.Y.M. Perfil de Resistência de Mycobacterium tuberculosis no Estado de São Paulo, 1986 a 1990. Rev. Inst. Adolfo Lutz, 52: 37-40, 1992.
34. SNIDER, D.E.Jr.; RAVIGLIONE, M. and KOCHI, A. Global burden of tuberculosis. In: Bloom, B.R (ed.) Tuberculosis: pathogenesis, protection and controI. American Society for Microbiology, Washington, n.c, 1st Ed., 1994, p. 3-11
35. TENOVER, F.e; CRAWFORD, J.T., HUEBNER, RE.; GEITER, L.J.; HORSBURGH Jr, C.R. and GOOD, R.C. The resurgence of Tuberculosis: Is your laboratory ready? J. CI. MicrobioI., 31: 767-70, 1993.
36. TOMAN, K. Tuberculosis: case-finding and chemotherapy. Questions and answers. World Health Organization, 1979.
37. TSUKAMURA, M. In vitro bacteriostatic and bactericidal activity of isoniazid on the
Mycobacterium avium-Mycobacterium intracellulare complexo Tubercle, 71:199-204,1990.
38. VIGORITA, M.G.; BASILE, M.; ZAPPALÀ, e; GABRIELLI, G. and PIZZIMENTI, F.
Halogenated isoniazid derivatives as possible antitubercular and antineoplastic agents. Note 1. 11Farmaco, 47: 893-903, 1992.
39. VISKUM, K. and JOK-JENSEN,A. Multidrug-resistant tuberculosis in Denmark 1993-1995. Int. J. Tuberc. Lung. Dis., 1: 299-301., 1997.
40. VOYATZAKIS, VA.E.; VASlLIKIOTIS, G.S.; KARAGEORGIOU, G. & KASSAPOGLOU, I.R lnfluence of metallic ions on the antituberculous activity of isonicotinoyl hydrazones. J. Pharm. Sci., 57: 1255-7, 1968.
41. WORLD HEALTH ORGANIZATION. WHO Report on the Tuberculosis Epidemic. Tuberculosis (TB) Annual Report - DOTS (Directly Observed Treatment, Short-course) A Breakthrough in TB Control, 40 p., 1997.
42. YAMAMOTO, S.; TOIDA, 1.; WATANABE, N. and URA, T. In vitro antimycobacterial activities of pyrazinamide analogs. Antimicrob. Agents Chemother., 39: 2088-91, 1995.
43. YEW, W.W. and CHAU, CH. Drug-resistant tuberculosis in the 1990s. Eur. Resp. J., 8: 1184-92, 1995.
44. YOUNG, D.B. Strategies for new drug development. ln: Bloom, B.R (ed.) Tuberculosis: Pathogenesis, Protection and Control. American Society for Microbiology, Washington, D.e, 1ST Ed., 1994, p. 559-567.
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Copyright (c) 1999 Instituto Adolfo Lutz Journal
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