title: Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. ping_chen@merck.com
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Charles G
authors.initials: CG
authors.lastname: Caldwell
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Mathvink
authors.forename: Barbara
authors.initials: B
authors.lastname: Leiting
authors.forename: Frank
authors.initials: F
authors.lastname: Marsilio
authors.forename: Reshma A
authors.initials: RA
authors.lastname: Patel
authors.forename: Joseph K
authors.initials: JK
authors.lastname: Wu
authors.forename: Huaibing
authors.initials: H
authors.lastname: He
authors.forename: Kathryn A
authors.initials: KA
authors.lastname: Lyons
authors.forename: Nancy A
authors.initials: NA
authors.lastname: Thornberry
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
mesh_terms: 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
chemical_list: D000577:Amides; D054873:Dipeptidyl-Peptidase IV Inhibitors; D007004:Hypoglycemic Agents; D010880:Piperidines; D011480:Protease Inhibitors