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The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists

✍ Scribed by Dale J. Johnson; Ian T. Forbes; Steve P. Watson; Vincenzo Garzya; Graeme I. Stevenson; Graham R. Walker; Harminder S. Mudhar; Sean T. Flynn; Paul A. Wyman; Paul W. Smith; Graham S. Murkitt; Adam J. Lucas; Claudette R. Mookherjee; Jeannette M. Watson; Jane E. Gartlon; Andrea M. Bradford; Fiona Brown

Book ID: 104004697
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 460 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.097

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✦ Synopsis

A series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles are reported which were found to be potent and selective muscarinic M1 agonists. By control of the physicochemical characteristics of the series, particularly the lipophilicity, compounds with good metabolic stability and excellent brain penetration were identified. An exemplar of the series was shown to be pro-cognitive in the novel object recognition rat model of temporal induced memory deficit.

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