The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines

被引：26

作者：

Albright, JD ^{[1
]}

Delos Santos, EG ^{[1
]}

Dusza, JP ^{[1
]}

Chan, PS ^{[1
]}

Coupet, J ^{[1
]}

Ru, X ^{[1
]}

Mazandarani, H ^{[1
]}

机构：

[1] Wyeth Ayerst Res, Chem Sci, Pearl River, NY 10965 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(00)00084-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis and SAR of N-[4-[(4, 5-dihydropyrazolo[3,4-D]thieno[3,2-b]azepin-6(2H)-yl)carbonyl]phenyl]benzamides as arginine vasopressin (AVP) receptor antagonists are discussed. Potent orally active AVP receptor antagonists are produced when the benzamide moietv contains a phenyl group at the 2-position. Similar analogues of 4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepine and VPA-985 are reported. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：695 / 698

页数：4

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