Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series

被引：24

作者：

Kuduk, Scott D. ^{[1
]}

Chang, Ronald K. ^{[1
]}

Di Marco, Christina N. ^{[1
]}

Ray, William J. ^{[2
]}

Ma, Lei ^{[2
]}

Wittmann, Marion ^{[2
]}

Seager, Matthew A. ^{[2
]}

Koeplinger, Kenneth A. ^{[3
]}

Thompson, Charles D. ^{[3
]}

Hartman, George D. ^{[1
]}

Bilodeau, Mark T. ^{[1
]}

机构：

[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA

[2] Merck Res Labs, Dept Alzheimers Res, West Point, PA 19486 USA

[3] Merck Res Labs, Dept Drug Metab, West Point, PA 19486 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 06期

关键词：

Allosteric; Modulator; Muscarinic; Quinolizidinone;

D O I：

10.1016/j.bmcl.2011.01.094

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

SAR study of the piperidine moiety in a series of quinolizidinone carboxylic acid M1 positive allosteric modulators was examined. While the SAR was generally flat, compounds were identified with high CNS exposure to warrant additional in vivo evaluation. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1710 / 1715

页数：6

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