title: Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
abstract: anti-Substituted beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. These are among the most potent compounds reported to date lacking an electrophilic trap. The most potent compound among these is 5-oxo-1,2,4-oxadiazole 44, which is a 3 nM DPP-IV inhibitor.
authors.affiliation: Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA.
authors.forename: Jinyou
authors.initials: J
authors.lastname: Xu
authors.forename: Lan
authors.initials: L
authors.lastname: Wei
authors.forename: Robert
authors.initials: R
authors.lastname: Mathvink
authors.forename: Jiafang
authors.initials: J
authors.lastname: He
authors.forename: You-Jung
authors.initials: YJ
authors.lastname: Park
authors.forename: Huaibing
authors.initials: H
authors.lastname: He
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: 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: D018819:Dipeptidyl Peptidase 4 / Q000187:drug effects*; D010649:Phenylalanine / Q000737:chemistry / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011480:Protease Inhibitors; D010649:Phenylalanine; D018819:Dipeptidyl Peptidase 4