The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives

被引：34
|
作者：
Tukulula, Matshawandile [1 ]
Little, Susan [2 ]
Gut, Jiri [3 ]
Rosenthal, Philip J. [3 ]
Wan, Baojie [4 ]
Franzblau, Scott G. [4 ]
Chibale, Kelly [1 ,5 ]
机构：
[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa
[2] London Sch Hyg & Trop Med, London WC1E 7HT, England
[3] Univ San Francisco, Dept Med, San Francisco Gen Hosp, San Francisco, CA 94143 USA
[4] Univ Illinois, Inst TB Res, Coll Pharm, Chicago, IL 60612 USA
[5] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 57卷
基金：
新加坡国家研究基金会;
关键词：
Antiplasmodial; Antimycobacterial; Arylamino quinoline tetrazoles; Physico-chemical properties; NONREPLICATING MYCOBACTERIUM-TUBERCULOSIS; CLEAVABLE ISOCYANIDES; CRYSTAL-STRUCTURE; TETRAZOLES; ACID; DISCOVERY; SERIES; AGENTS; TMC207; ASSAY;
D O I：
10.1016/j.ejmech.2012.08.047
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of new arylamino quinoline derivatives was designed based on the quinine and mefloquine scaffolds and evaluated in vitro for antiplasmodial and antimycobacterial activities. A number of these compounds exhibited significant activity against the drug-sensitive 3D7 and drug-resistant K1 strains of Plasmodium falciparum. Furthermore, two compounds, 4.12b and 4.12d, also showed 94 and 98% growth inhibitory activity against non-replicating and replicating Mycobacterium tuberculosis strains, respectively. (C) 2012 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：259 / 267
页数：9
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