Diphenylsulfone muscarinic antagonists:: Piperidine derivatives with high M2 selectivity and improved potency

被引：16

作者：

Billard, W ^{[1
]}

Binch, H ^{[1
]}

Bratzler, K ^{[1
]}

Chen, LY ^{[1
]}

Crosby, G ^{[1
]}

Duffy, RA ^{[1
]}

Dugar, S ^{[1
]}

Lachowicz, J ^{[1
]}

McQuade, R ^{[1
]}

Pushpavanam, P ^{[1
]}

Ruperto, VB ^{[1
]}

Taylor, LA ^{[1
]}

Clader, JW ^{[1
]}

机构：

[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(00)00437-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Piperidine analogues of our previously described piperazine muscarinic antagonists are described. Piperidine analogues show a distinct structure-activity relationship (SAR) that differs from comparable piperazines. Compounds with high selectivity and improved potency for the M-2 receptor have been identified. The lead compound, 12b, increases acetylcholine release in vivo. Compounds of this class may be useful for the treatment of cognitive disorders such as Alzheimer's disease (AD). (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2209 / 2212

页数：4

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