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

被引：287

作者：

Boechat, Nubia ^{[1
]}

Ferreira, Vitor F. ^{[2
]}

Ferreira, Sabrina B. ^{[2
]}

Ferreira, Maria de Lourdes G. ^{[1
]}

da Silva, Fernando de C. ^{[2
]}

Bastos, Monica M. ^{[1
]}

Costa, Marilia dos S. ^{[1
]}

Lourenco, Maria Cristina S. ^{[2
]}

Pinto, Angelo C. ^{[3
]}

Krettli, Antoniana U. ^{[4
]}

Aguiar, Anna Caroline ^{[4
]}

Teixeira, Brunno M. ^{[2
]}

da Silva, Nathalia V. ^{[2
]}

Martins, Priscila R. C. ^{[2
]}

Bezerra, Flavio Augusto F. M. ^{[2
]}

Camilo, Ane Louise S. ^{[1
]}

da Silva, Gerson P. ^{[1
,3
]}

Costa, Carolina C. P. ^{[1
]}

机构：

[1] Fundacao Oswaldo Cruz, Inst Tecnol Farmacos, Dept Sintese Organ, BR-21041250 Rio De Janeiro, Brazil

[2] Fundacao Oswaldo Cruz, Inst Pesquisa Clin Evandro Chagas IPEC, Lab Bacteriol & Bioensaios Micobacterias, BR-21045900 Rio De Janeiro, Brazil

[3] Univ Fed Rio de Janeiro, Inst Quim, Dept Quim Organ, BR-21941909 Rio De Janeiro, Brazil

[4] Fundacao Oswaldo Cruz, Lab Malaria, Ctr Pesquisas Rene Rachou, BR-30190002 Belo Horizonte, MG, Brazil

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 54卷 / 17期

关键词：

IN-VITRO; CELL-GROWTH; ACID; RESISTANT; SUSCEPTIBILITY; RIFAMPIN; ASSAY; VIVO; C-4;

D O I：

10.1021/jm2003624

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu g/mL (mu M). 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 mu g/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.

引用

页码：5988 / 5999

页数：12

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