期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 18, 页码 5434-5438出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.097
关键词
Muscarinic M-1 agonist; Cognitive enhancer; Allosteric; Central nervous system penetration; Benzoxazolinone; Oxidole
A series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles are reported which were found to be potent and selective muscarinic M-1 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. (c) 2010 Elsevier Ltd. All rights reserved.
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