Antitubercular Activity of New Coumarins

被引：54

作者：

Cardoso, Silvia H. ^{[2
]}

Barreto, Milena B. ^{[3
]}

Lourenco, Maria C. S. ^{[4
]}

Henriques, Maria das Gracas M. de O. ^{[1
]}

Candea, Andre L. P. ^{[1
]}

Kaiser, Carlos R. ^{[3
]}

de Souza, Marcus V. N. ^{[1
]}

机构：

[1] Fundacao Oswaldo Cruz, Inst Tecnol Farmacos Far Manguinhos, BR-21041250 Rio De Janeiro, Brazil

[2] Univ Fed Alagoas, BR-57309005 Arapiraca, AL, Brazil

[3] Univ Fed Rio de Janeiro, Dept Quim Organ, Inst Quim, BR-21945970 Rio De Janeiro, Brazil

[4] Inst Pesquisas Clin Evandro Chagas IPEC, BR-4365 Rio De Janeiro, Brazil

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2011年 / 77卷 / 06期

关键词：

coumarins; drugs; N'-acylhydrazones; tuberculosis; DERIVATIVES;

D O I：

10.1111/j.1747-0285.2011.01120.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The present article describes a series of 21 N '-benzylidene-2-oxo-2H-chromene-3-carbohydrazides 4a-4v, which were synthesized and evaluated for their cell viabilities in non-infected and Mycobacterium bovis Bacillus Calmette-Guerin-infected macrophages. Subsequently, the non-cytotoxic compounds 4c, 4g, 4h, 4j, 4l and 4t were assessed against Mycobacterium tuberculosis ATCC 27294 using the microplate Alamar Blue assay and the activity expressed as the minimum inhibitory concentration in mu g/mL. These compounds exhibited a significant activity (50-100 mu g/mL) when compared to the first-line drugs, such as pyrazinamide (PZA > 100 mu g/mL). These results could be considered a good starting point for further studies to develop new lead compounds to treat multidrug-resistant tuberculosis.

引用

页码：489 / 493

页数：5

共 34 条

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