Novel 1,2,3-Triazole Derivatives for Use against <i>Mycobacterium tuberculosis</i> H37Rv (ATCC 27294) Strain

Núbia Boechat(Fundação Oswaldo Cruz), Vı́tor F. Ferreira(Fundação Oswaldo Cruz), Sabrina Baptista Ferreira(Fundação Oswaldo Cruz), M.De L. Ferreira(Fundação Oswaldo Cruz), Fernando de Carvalho da Silva(Fundação Oswaldo Cruz), Mônica M. Bastos(Fundação Oswaldo Cruz), Marilia dos S. Costa(Fundação Oswaldo Cruz), Maria Cristina S. Lourenço(Fundação Oswaldo Cruz), Ângelo C. Pinto(Universidade Federal do Rio de Janeiro), Antoniana U. Krettli(Fundação Oswaldo Cruz), Anna Caroline Campos Aguiar(Fundação Oswaldo Cruz), Brunno M. Teixeira(Fundação Oswaldo Cruz), Nathalia V. da Silva(Fundação Oswaldo Cruz), Priscila Raquel Martins(Fundação Oswaldo Cruz), Flávio A. F. M. Bezerra(Fundação Oswaldo Cruz), A.L.S. Camilo(Fundação Oswaldo Cruz), Gerson P. da Silva(Universidade Federal do Rio de Janeiro), Carolina C. P. Costa(Fundação Oswaldo Cruz)
Journal of Medicinal Chemistry
July 21, 2011
Cited by 282

Abstract

The purpose of this study was to prepare various 4-substituted N-phenyl-1,2,3-triazole derivatives using click chemistry. The derivatives were screened in vitro for antimicrobial activity against Mycobacterium tuberculosis strain H37Rv (ATCC 27294) using the Alamar Blue susceptibility test. The activity was expressed as the minimum inhibitory concentration (MIC) in μg/mL (μM). Derivatives of isoniazid (INH), (E)-N'-[(1-aryl)-1H-1,2,3-triazole-4-yl)methylene] isonicotinoyl hydrazides, exhibited significant activity with MIC values ranging from 2.5 to 0.62 μg/mL. In addition, they displayed low cytotoxicity against liver cells (hepatoma HepG2) and kidney cells (BGM), thereby providing a high therapeutic index. The results demonstrated the potential and importance of developing new INH derivatives to treat mycobacterial infections.


Related Papers

No related papers found

Powered by citation graph analysis