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

页码：259 / 267

页数：9

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