Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase.: Modifications at positions 5′ and 8

被引：15

作者：

Aronov, AM

Gelb, MH ^{[1
]}

机构：

[1] Univ Washington, Dept Chem, Seattle, WA 98195 USA

[2] Univ Washington, Dept Biochem, Seattle, WA 98195 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 24期

关键词：

D O I：

10.1016/S0960-894X(98)00635-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A number of 5', N-6- and C-8, N-6-disubstituted adenosine analogs was synthesized and tested for inhibition of trypanosomal glyceraldehyde 3-phosphate dehydrogenase. The most active compound, N-6-(3-methyl-2-butenyl)-8-(2-thienyl)adenosine had K-l of 9 mu M and was marginally selective for the parasite enzyme. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：3505 / 3510

页数：6

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