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Bioorg Med Chem Lett. 2010 Sep 15;20(18):5434-8. doi: 10.1016/j.bmcl.2010.07.097. Epub 2010 Jul 30.

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

Author information

1
GlaxoSmithKline, New Frontiers Science Park, 3rd Avenue, Harlow, Essex CM19 5AW, UK. dalejames.johnson@gmail.com

Abstract

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.

PMID:
20709550
DOI:
10.1016/j.bmcl.2010.07.097
[Indexed for MEDLINE]

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