title: Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones.
abstract: Synthesis of a novel series of DPPIV inhibitors with 1,2,4- and 1,3,4-oxadiazolyl ketone derivatives and its structure-activity relationships are discussed. Compound 18h showed good inhibitory activity against DPPIV and favorable pharmacokinetic properties. In vivo pharmacodynamic efficacy and co-crystal structure of compound 18h with DPPIV is also described.
authors.affiliation: LG Life Sciences, Ltd/R&D Park, 104-1 Munji-dong, Yuseong-gu, Daejeon 305-380, Republic of Korea.
authors.forename: Ki Dong
authors.initials: KD
authors.lastname: Koo
authors.forename: Min Jung
authors.initials: MJ
authors.lastname: Kim
authors.forename: Sungsub
authors.initials: S
authors.lastname: Kim
authors.forename: Kyoung-Hee
authors.initials: KH
authors.lastname: Kim
authors.forename: Sang Yong
authors.initials: SY
authors.lastname: Hong
authors.forename: Gwong-Cheung
authors.initials: GC
authors.lastname: Hur
authors.forename: Hyeon Joo
authors.initials: HJ
authors.lastname: Yim
authors.forename: Geun Tae
authors.initials: GT
authors.lastname: Kim
authors.forename: Hee Oon
authors.initials: HO
authors.lastname: Han
authors.forename: O Hwan
authors.initials: OH
authors.lastname: Kwon
authors.forename: Tae Sik
authors.initials: TS
authors.lastname: Kwon
authors.forename: Jong Sung
authors.initials: JS
authors.lastname: Koh
authors.forename: Chang-Seok
authors.initials: CS
authors.lastname: Lee
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D018819:Dipeptidyl Peptidase 4 / Q000378:metabolism; D054873:Dipeptidyl-Peptidase IV Inhibitors; D004285:Dogs; D000882:Haplorhini; D007659:Ketones / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D054873:Dipeptidyl-Peptidase IV Inhibitors; D007659:Ketones; D011480:Protease Inhibitors; D018819:Dipeptidyl Peptidase 4