Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.
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.
Rosauer
Keith G
KG
Department of Basic Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. keith_rosauer@merck.com
Ogawa
Anthony K
AK
Willoughby
Chris A
CA
Ellsworth
Kenneth P
KP
Geissler
Wayne M
WM
Myers
Robert W
RW
Deng
Qiaolin
Q
Chapman
Kevin T
KT
Harris
Georgianna
G
Moller
David E
DE
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
D004791:Enzyme Inhibitors; D011804:Quinolines; D024981:Glycogen Phosphorylase