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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Kuduk, Scott D.¹  Chang, Ronald K.¹  Di Marco, Christina N.¹  Ray, William J.²  Ma, Lei²  Wittmann, Marion²  Seager, Matthew A.²  Koeplinger, Kenneth A.³  Thompson, Charles D.³  Hartman, George D.¹  Bilodeau, Mark T.¹ 

[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

关键词: Allosteric;    Modulator;    Muscarinic;    Quinolizidinone;   

DOI  :  10.1016/j.bmcl.2011.01.094

来源: Elsevier

【 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.

【 授权许可】

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