title: Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
abstract: Various beta-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. jennifer_kowalchick@yahoo.com
authors.forename: Jennifer E
authors.initials: JE
authors.lastname: Kowalchick
authors.forename: Barbara
authors.initials: B
authors.lastname: Leiting
authors.forename: KellyAnn D
authors.initials: KD
authors.lastname: Pryor
authors.forename: Frank
authors.initials: F
authors.lastname: Marsilio
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: George J
authors.initials: GJ
authors.lastname: Eiermann
authors.forename: Aleksandr
authors.initials: A
authors.lastname: Petrov
authors.forename: Giovanna
authors.initials: G
authors.lastname: Scapin
authors.forename: Reshma A
authors.initials: RA
authors.lastname: Patel
authors.forename: Nancy A
authors.initials: NA
authors.lastname: Thornberry
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
authors.forename: Dooseop
authors.initials: D
authors.lastname: Kim
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D018360:Crystallography, X-Ray; D054873:Dipeptidyl-Peptidase IV Inhibitors; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D008958:Models, Molecular; D010879:Piperazines / Q000737:chemistry*; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats