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Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators.

ABSTRACT: Selective activation of the M1 muscarinic receptor via positive allosteric modulation represents an original approach to treat the cognitive decline in patients with Alzheimer's disease. A series of naphthyl-fused 5-membered lactams were identified as a new class of M1 positive allosteric modulators and were found to possess good potency and in vivo efficacy.

SUBMITTER: Yang ZQ

PROVIDER: S-EPMC4027734 | biostudies-literature | 2014 May

REPOSITORIES: biostudies-literature

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Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators.

Yang Zhi-Qiang ZQ Shu Youheng Y Ma Lei L Wittmann Marion M Ray William J WJ Seager Matthew A MA Koeplinger Kenneth A KA Thompson Charles D CD Hartman George D GD Bilodeau Mark T MT Kuduk Scott D SD

ACS medicinal chemistry letters 20140220 5

Selective activation of the M1 muscarinic receptor via positive allosteric modulation represents an original approach to treat the cognitive decline in patients with Alzheimer's disease. A series of naphthyl-fused 5-membered lactams were identified as a new class of M1 positive allosteric modulators and were found to possess good potency and in vivo efficacy. ...[more]

PMID: 24900888

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