Discovery and SAR development of 2-(phenylamino) imidazolines as postacyclin receptor antagonists

被引：50

作者：

Clark, RD

Jahangir, A

Severance, D

Salazar, R

Chang, T

Chang, D

Jett, MF

Smith, S

Bley, K

机构：

[1] Roche Palo Alto, Dept Med Chem, Palo Alto, CA 94304 USA

[2] Roche Palo Alto, Dept Pharmacol, Palo Alto, CA 94304 USA

[3] Roche Palo Alto, Dept Drug Metab & Pharmacokinet, Palo Alto, CA 94304 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 04期

关键词：

D O I：

10.1016/j.bmcl.2003.10.070

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

On the basis of screening hits (1a,b), a series of selective, high affinity prostacyclin receptor antagonists was developed. The optimized lead compound 25d [(4,5-dihydro-1H-imidazol-2-yl)-[4-(4-isopropoxybenzyl)phenyl]amine] had analgesic activity in the rat. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：1053 / 1056

页数：4

共 16 条

[1] PRODUCTION OF PROSTACYCLIN IN MICE FOLLOWING INTRAPERITONEAL INJECTION OF ACETIC-ACID, PHENYLBENZOQUINONE AND ZYMOSAN - ITS ROLE IN THE WRITHING RESPONSE [J].