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.
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收藏
页码：967 / 972
页数：6
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[11]   Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists [J].
Wustrow, DJ ;
Capiris, T ;
Rubin, R ;
Knobelsdorf, JA ;
Akunne, H ;
Davis, MD ;
MacKenzie, R ;
Pugsley, TA ;
Zoski, KT ;
Heffner, TG ;
Wise, LD .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (16) :2067-2070
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