Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists

被引：40

作者：

Beck, JP

Arvanitis, AG

Curry, MA

Rescinito, JT

Fitzgerald, LW

Gilligan, PJ

Zaczek, R

Trainor, GL

机构：

[1] Dupont Co, Chem & Phys Sci, Wilmington, DE 19880 USA

[2] Dupont Co, CNS Dis Res Expt Stn, Wilmington, DE 19880 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(99)00108-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of purin-8-ones was prepared and discovered to have excellent binding affintity to the CRH-R1 receptor. Structure-activity studies focused on amine side-chain optimization, urea substitution and pyridyl isostere incorporation. Thus, the highly potent purin-8-ones show promise as a new class of potential anxiolytics and/or antidepressants. (C) 1999 DuPont Pharmaceuticals. Published by Elsevier Science I,td. All rights reserved.

引用

页码：967 / 972

页数：6

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