title: Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
abstract: An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M(1) positive allosteric modulators, and strategies for improving potency and plasma free fraction were identified.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
authors.forename: Feng V
authors.initials: FV
authors.lastname: Yang
authors.forename: William D
authors.initials: WD
authors.lastname: Shipe
authors.forename: Jaime L
authors.initials: JL
authors.lastname: Bunda
authors.forename: M Brad
authors.initials: MB
authors.lastname: Nolt
authors.forename: David D
authors.initials: DD
authors.lastname: Wisnoski
authors.forename: Zhijian
authors.initials: Z
authors.lastname: Zhao
authors.forename: James C
authors.initials: JC
authors.lastname: Barrow
authors.forename: William J
authors.initials: WJ
authors.lastname: Ray
authors.forename: Lei
authors.initials: L
authors.lastname: Ma
authors.forename: Marion
authors.initials: M
authors.lastname: Wittmann
authors.forename: Matthew A
authors.initials: MA
authors.lastname: Seager
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Koeplinger
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Craig W
authors.initials: CW
authors.lastname: Lindsley
mesh_terms: D000494:Allosteric Regulation; D000818:Animals; D001798:Blood Proteins / Q000737:chemistry / Q000378:metabolism; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D011485:Protein Binding; D011804:Quinolines / Q000737:chemistry*; D051381:Rats; D043643:Receptor, Muscarinic M1 / Q000378:metabolism*; D054852:Small Molecule Libraries
chemical_list: D001798:Blood Proteins; D002264:Carboxylic Acids; D011804:Quinolines; D043643:Receptor, Muscarinic M1; D054852:Small Molecule Libraries