Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
A series of substituted imidazopiperidine amides has been prepared and evaluated for inhibition of dipeptidyl peptidase IV (DPP-4). Substitution at the 1- and 3-positions produced increased selectivity for DPP-4 relative to DPP-8 and DPP-9. Compounds in this series had IC(50) values as low as 5.8 nM for inhibition of DPP-4.
Chen
Ping
P
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. ping_chen@merck.com
Caldwell
Charles G
CG
Mathvink
Robert J
RJ
Leiting
Barbara
B
Marsilio
Frank
F
Patel
Reshma A
RA
Wu
Joseph K
JK
He
Huaibing
H
Lyons
Kathryn A
KA
Thornberry
Nancy A
NA
Weber
Ann E
AE
D000577:Amides / Q000737:chemistry; D003920:Diabetes Mellitus / Q000188:drug therapy*; D054873:Dipeptidyl-Peptidase IV Inhibitors; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use
D000577:Amides; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D010880:Piperidines; D011480:Protease Inhibitors