A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase

被引：41

作者：

Kennedy, KJ

Bressi, JC

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 | 2001年 / 11卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(00)00608-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-6-Naphthalenemethyl-2'-methoxybenzamido-beta -NAD(+), a derivative of a low micromolar first-generation inhibitor of trypanosomal glyceraldehyde phosphate dehydrogenase (GAPDH), was synthesized, taking advantage of methodology for the selective phosphitylation of nucleosides. The compound was found to be a poor alternate cosubstrate for GAPDH, but an extremely potent inhibitor. Although intended for use in crystallization trials, the analogue presents possibilities for further drug design. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：95 / 98

页数：4

共 12 条

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