title: Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
abstract: The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-(S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of dipeptidyl peptidase IV (DPP IV) are reported.
authors.affiliation: Johnson and Johnson Pharmaceutical Research and Development, 665 Stockton Drive, Exton, PA 19341, USA.
authors.forename: Lei
authors.initials: L
authors.lastname: Qiao
authors.forename: Christian A
authors.initials: CA
authors.lastname: Baumann
authors.forename: Carl S
authors.initials: CS
authors.lastname: Crysler
authors.forename: Nisha S
authors.initials: NS
authors.lastname: Ninan
authors.forename: Marta C
authors.initials: MC
authors.lastname: Abad
authors.forename: John C
authors.initials: JC
authors.lastname: Spurlino
authors.forename: Renee L
authors.initials: RL
authors.lastname: Desjarlais
authors.forename: Jukka
authors.initials: J
authors.lastname: Kervinen
authors.forename: Mike P
authors.initials: MP
authors.lastname: Neeper
authors.forename: Shariff S
authors.initials: SS
authors.lastname: Bayoumy
authors.forename: Robyn
authors.initials: R
authors.lastname: Williams
authors.forename: Ingrid C
authors.initials: IC
authors.lastname: Deckman
authors.forename: Malini
authors.initials: M
authors.lastname: Dasgupta
authors.forename: Rolanda L
authors.initials: RL
authors.lastname: Reed
authors.forename: Norman D
authors.initials: ND
authors.lastname: Huebert
authors.forename: Bruce E
authors.initials: BE
authors.lastname: Tomczuk
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Moriarty
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D001665:Binding Sites; D001786:Blood Glucose / Q000378:metabolism; D018938:Caco-2 Cells; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods*; D018819:Dipeptidyl Peptidase 4 / Q000737:chemistry* / Q000378:metabolism; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D051379:Mice; D008956:Models, Chemical; D008958:Models, Molecular; D011480:Protease Inhibitors / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001786:Blood Glucose; D004791:Enzyme Inhibitors; D011480:Protease Inhibitors; D018819:Dipeptidyl Peptidase 4