Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7

被引：35

作者：

Bouloc, Nathalie ^{[1
]}

Large, Jonathan M. ^{[1
]}

Smiljanic, Ela ^{[1
]}

Whalley, David ^{[1
]}

Ansell, Keith H. ^{[1
]}

Edlin, Christopher D. ^{[1
]}

Bryans, Justin S. ^{[1
]}

机构：

[1] MRC Technol, Drug Discovery Grp, London NW7 1AD, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 19期

关键词：

malaria; kinase inhibitors; imidazopyridazines;

D O I：

10.1016/j.bmcl.2008.08.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5294 / 5298

页数：5

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