title: Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain.
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.
authors.affiliation: Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos, Departamento de Síntese Orgânica, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil. boechat@far.fiocruz.br
authors.forename: Nubia
authors.initials: N
authors.lastname: Boechat
authors.forename: Vitor F
authors.initials: VF
authors.lastname: Ferreira
authors.forename: Sabrina B
authors.initials: SB
authors.lastname: Ferreira
authors.forename: Maria
authors.initials: M
authors.lastname: de Lourdes G Ferreira
authors.forename: Fernando
authors.initials: F
authors.lastname: de C da Silva
authors.forename: Monica M
authors.initials: MM
authors.lastname: Bastos
authors.forename: Marilia
authors.initials: M
authors.lastname: Dos S Costa
authors.forename: Maria Cristina S
authors.initials: MC
authors.lastname: Lourenço
authors.forename: Angelo C
authors.initials: AC
authors.lastname: Pinto
authors.forename: Antoniana U
authors.initials: AU
authors.lastname: Krettli
authors.forename: Anna Caroline
authors.initials: AC
authors.lastname: Aguiar
authors.forename: Brunno M
authors.initials: BM
authors.lastname: Teixeira
authors.forename: Nathalia V
authors.initials: NV
authors.lastname: da Silva
authors.forename: Priscila R C
authors.initials: PR
authors.lastname: Martins
authors.forename: Flavio Augusto F M
authors.initials: FA
authors.lastname: Bezerra
authors.forename: Ane Louise S
authors.initials: AL
authors.lastname: Camilo
authors.forename: Gerson P
authors.initials: GP
authors.lastname: da Silva
authors.forename: Carolina C P
authors.initials: CC
authors.lastname: Costa
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy*; D049109:Cell Proliferation / Q000187:drug effects*; D057930:Click Chemistry; D006801:Humans; D007538:Isoniazid / Q000737:chemistry*; D008113:Liver Neoplasms / Q000188:drug therapy*; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000995:Antitubercular Agents; D014230:Triazoles; D007538:Isoniazid