title: Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
abstract: A novel series of oxadiazole based amides have been shown to be potent DPP-4 inhibitors. The optimized compound 43 exhibited excellent selectivity over a variety of DPP-4 homologs.
authors.affiliation: Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. Jinyou_Xu@merck.com
authors.forename: Jinyou
authors.initials: J
authors.lastname: Xu
authors.forename: Lan
authors.initials: L
authors.lastname: Wei
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Mathvink
authors.forename: Scott D
authors.initials: SD
authors.lastname: Edmondson
authors.forename: George J
authors.initials: GJ
authors.lastname: Eiermann
authors.forename: Huaibing
authors.initials: H
authors.lastname: He
authors.forename: Joseph F
authors.initials: JF
authors.lastname: Leone
authors.forename: Barbara
authors.initials: B
authors.lastname: Leiting
authors.forename: Kathryn A
authors.initials: KA
authors.lastname: Lyons
authors.forename: Frank
authors.initials: F
authors.lastname: Marsilio
authors.forename: Reshma A
authors.initials: RA
authors.lastname: Patel
authors.forename: Sangita B
authors.initials: SB
authors.lastname: Patel
authors.forename: Aleksandr
authors.initials: A
authors.lastname: Petrov
authors.forename: Giovanna
authors.initials: G
authors.lastname: Scapin
authors.forename: Joseph K
authors.initials: JK
authors.lastname: Wu
authors.forename: Nancy A
authors.initials: NA
authors.lastname: Thornberry
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001665:Binding Sites; D001682:Biological Availability; D054873:Dipeptidyl-Peptidase IV Inhibitors; D004285:Dogs; D004789:Enzyme Activation / Q000187:drug effects; D051638:Ether-A-Go-Go Potassium Channels / Q000187:drug effects; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D010069:Oxadiazoles / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D051638:Ether-A-Go-Go Potassium Channels; D010069:Oxadiazoles; D011480:Protease Inhibitors