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

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.

journal_name

Bioorg Med Chem Lett

authors

Johnson DJ,Forbes IT,Watson SP,Garzya V,Stevenson GI,Walker GR,Mudhar HS,Flynn ST,Wyman PA,Smith PW,Murkitt GS,Lucas AJ,Mookherjee CR,Watson JM,Gartlon JE,Bradford AM,Brown F

doi

10.1016/j.bmcl.2010.07.097

subject

Has Abstract

pub_date

2010-09-15 00:00:00

pages

5434-8

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01066-8

journal_volume

20

pub_type

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