title: 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.
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Zhi-Qiang
authors.initials: ZQ
authors.lastname: Yang
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Youheng
authors.initials: Y
authors.lastname: Shu
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Lei
authors.initials: L
authors.lastname: Ma
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Marion
authors.initials: M
authors.lastname: Wittmann
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: William J
authors.initials: WJ
authors.lastname: Ray
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Matthew A
authors.initials: MA
authors.lastname: Seager
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Koeplinger
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Charles D
authors.initials: CD
authors.lastname: Thompson
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Mark T
authors.initials: MT
authors.lastname: Bilodeau
authors.affiliation: Departments of Medicinal Chemistry, Alzheimer's Research, and Drug Metabolism, Merck Research Laboratories , Sumneytown Pike, West Point, Pennsylvania 19486, United States.
authors.forename: Scott D
authors.initials: SD
authors.lastname: Kuduk
keywords: Alzheimer’s disease; M1; acetylcholine; muscarinic; positive allosteric modulators