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Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain.
J Med Chem ; 54(17): 5988-99, 2011 Sep 08.
Article en En | MEDLINE | ID: mdl-21776985
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Contexto en salud: 3_ND Problema de salud: 3_neglected_diseases / 3_tuberculosis Asunto principal: Triazoles / Carcinoma Hepatocelular / Proliferación Celular / Isoniazida / Neoplasias Hepáticas / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2011 Tipo del documento: Article País de afiliación: Brasil

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Contexto en salud: 3_ND Problema de salud: 3_neglected_diseases / 3_tuberculosis Asunto principal: Triazoles / Carcinoma Hepatocelular / Proliferación Celular / Isoniazida / Neoplasias Hepáticas / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2011 Tipo del documento: Article País de afiliación: Brasil
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