Evaluation of anti-tubercular activity of nicotinic and isoniazid analogues

被引:227
|
作者
Lourenco, Maria C. S. [2 ]
Souza, Marcus V. N. de [1 ]
Pinheiro, Alessandra C. [1 ]
Ferreira, Marcelle de L. [1 ]
Goncalves, Raoni S. B. [1 ]
Nogueira, Thais Cristina M. [1 ]
Peralta, Monica A. [1 ]
机构
[1] FioCruz Fdn Oswaldo Cruz, Inst Tecnol & Farmacos Far Manguinhos, Rua Sizenando Nabuco 100, BR-21041250 Rio De Janeiro, Brazil
[2] Inst Pesquisas Clin Evandro Chagas, Dept Bacteriol, Rio De Janeiro, Brazil
关键词
tuberculosis; isoniazid; nicotinic acid; analogs;
D O I
10.3998/ark.5550190.0008.f18
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Several nicotinic and isoniazid derivatives, most of them containing nitro groups were synthesized by our group, and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H(37)Rv using the Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory concentration ( MIC) in mg/mL. The compound 11d exhibited the best result (1.2 mu g/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore this class of compounds could be a good starting point to develop new lead compounds in the treatment of multi-drug resistant tuberculosis.
引用
收藏
页码:181 / 191
页数:11
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