Identification of potent and selective oxytocin antagonists. Part 1: Indole and benzofuran derivatives

被引：33

作者：

Wyatt, PG

Allen, MJ

Chilcott, J

Foster, A

Livermore, DG

Mordaunt, JE

Scicinski, J

Woollard, PM

机构：

[1] GlaxoSmithKline, Med Res Ctr, Dept Med Chem, Stevenage SG1 2NY, Herts, England

[2] GlaxoSmithKline, Med Res Ctr, Dept Receptor Pharmacol, Stevenage SG1 2NY, Herts, England

[3] GlaxoSmithKline, Med Res Ctr, Dept Res Biometab, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(02)00159-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Studies to discover novel, potent and selective oxytocin antagonists are reported. Combinatorial libraries designed to End novel replacements of fragments of oxytocin antagonist L-371,257, identified pyrimidine, thiazole, indole and benzofuran as potential alternatives to the benzoic acid moiety of L-371,257. Additional investigations identified indole and benzofuran derivatives with potent oxytocin antagonist activity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1399 / 1404

页数：6

共 16 条

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ALLEN MB, IN PRESS

[2] A convenient procedure for the solution phase preparation of 2-aminothiazole combinatorial libraries [J].