title: Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.
abstract: The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
authors.affiliation: Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. keith_rosauer@merck.com
authors.forename: Keith G
authors.initials: KG
authors.lastname: Rosauer
authors.forename: Anthony K
authors.initials: AK
authors.lastname: Ogawa
authors.forename: Chris A
authors.initials: CA
authors.lastname: Willoughby
authors.forename: Kenneth P
authors.initials: KP
authors.lastname: Ellsworth
authors.forename: Wayne M
authors.initials: WM
authors.lastname: Geissler
authors.forename: Robert W
authors.initials: RW
authors.lastname: Myers
authors.forename: Qiaolin
authors.initials: Q
authors.lastname: Deng
authors.forename: Kevin T
authors.initials: KT
authors.lastname: Chapman
authors.forename: Georgianna
authors.initials: G
authors.lastname: Harris
authors.forename: David E
authors.initials: DE
authors.lastname: Moller
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors*; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011804:Quinolines; D024981:Glycogen Phosphorylase