SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents

被引：28

作者：

Gigante, Federica ^{[1
,2
]}

Kaiser, Marcel ^{[3
]}

Brun, Reto ^{[3
]}

Gilbert, Ian H. ^{[1
,2
]}

机构：

[1] Univ Dundee, Coll Life Sci, Sir James Black Ctr, Dundee DD1 5EH, Scotland

[2] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales

[3] Swiss Trop Inst, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 16期

关键词：

Trypanosomiasis; Leishmaniasis; Azasterols; DELTA-24-STEROL METHYLTRANSFERASE; TRYPANOSOMA-BRUCEI; CANDIDA-ALBICANS; SQUALAMINE; DERIVATIVES; INHIBITION; ANALOGS;

D O I：

10.1016/j.bmc.2009.06.062

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

There is an urgent need for the development of new drugs for the treatment of neglected tropical diseases such as human African trypanosomiasis, Chagas disease and leishmaniasis. Azasterols, have been shown to have activity against the parasites which cause these diseases. In this paper we report synthesis of new azasterols and subsequent analysis of the SAR. The chemistry focused on variations in the ester at the 3 beta-position of the sterol and the position of the nitrogen in the side chain. The data allowed us to derive preliminary pharmacophore models for the activity of the azasterols against the parasites which cause these diseases. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5950 / 5961

页数：12

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