A novel microwave synthesis of quinoline-3-carboxylic acid derivatives for treatment against human African trypanosomiasis

被引：0

作者：

Samant, Bhupesh S. ^{[1
]}

Nyangari, Nyaradzai ^{[1
]}

机构：

[1] Rhodes Univ, Nat Prod & Med Chem NPMC Res Grp, Div Pharmaceut Chem, Fac Pharm, ZA-6140 Grahamstown, South Africa

来源：

MOLECULAR DIVERSITY | 2012年 / 16卷 / 04期

关键词：

Human African trypanosomiasis; Quinoline-3-carboxylic acids; Sleeping sickness; Microwave irradiation; INFECTIONS;

D O I：

10.1007/s11030-012-9401-2

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 quinoline-3-carboxylic acid derivatives has been synthesized with easy reaction conditions (in aqueous micellar microreactors and using microwave irradiation) and tested for its biological activity against human African trypanosomiasis (HAT). From this series, several derivatives of quinoline-3-carboxylic acid such as 23 and 24 exhibited potent activity against Trypanosoma brucei in vitro and had low cytotoxicity. The combination of electron withdrawing and donating groups in the structure seems to be the crucial factor to inhibit T. brucei.

引用

页码：685 / 695

页数：11

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