Synthesis and in vitro antitubercular activity of a series of quinoline derivatives

被引：153

作者：

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

Pais, Karla C. ^{[1
,2
]}

Kaiser, Carlos R. ^{[2
]}

Peralta, Monica A. ^{[1
]}

Ferreira, Marcelle de L. ^{[1
,2
]}

Lourenco, Maria C. S. ^{[3
]}

机构：

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

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

[3] IPEC, Inst Pesquisas Clin Evandro Chagas, Rio De Janeiro, Brazil

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 04期

关键词：

Quinoline; Drugs; MDR-TB; Antitubercular activity; ALAMAR BLUE ASSAY; MYCOBACTERIUM-TUBERCULOSIS; PULMONARY TUBERCULOSIS; SIDE-CHAIN; 4-AMINOQUINOLINE; CHLOROQUINE; DESIGN; AGENTS; ACID; SUSCEPTIBILITY;

D O I：

10.1016/j.bmc.2009.01.013

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：

A series of 33 quinoline derivatives have been synthesized 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 mu g/mL. Compounds 5e and 5f exhibited a significant activity at 6.25 and 3.12 mu g/mL, respectively, when compared with first line drugs such as ethambutol and could be a good starting point to develop new lead compounds in the fight against multidrug resistant tuberculosis. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1474 / 1480

页数：7

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