New acetylene based histamine H2 receptor antagonists derived from the marine natural product verongamine

被引：13

作者：

Ali, SM ^{[1
]}

Tedford, CE ^{[1
]}

Gregory, R ^{[1
]}

Yates, SL ^{[1
]}

Phillips, JG ^{[1
]}

机构：

[1] Gliatech Inc, Cleveland, OH 44122 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(98)00181-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New histamine H-3 receptor antagonists were developed using an acetylene moiety as a replacement or the amide-oxime functionality of verongamine 5. Optimization of receptor binding was performed by following aliphatic Topliss tree guidelines. These new H-3 ligands demonstrate excellent blood-brain barrier penetration. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1133 / 1138

页数：6

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