title: Lead discovery of quinoxalinediones as an inhibitor of dipeptidyl peptidase-IV (DPP-IV) by high-throughput screening.
abstract: N-Ureido-quinoxalinedione derivatives have been discovered as leads for a novel series of dipeptidyl peptidase-IV (DPP-IV) inhibitors through high-throughput screening of our chemical library. A brief structure-activity relationship of the compounds was investigated. Among them, entry 5 showed the most potent inhibitory activity. The nitro group in quinoxaline moiety and the aromatic sulfonyl substituted ureido functional group seem to be important to increase the potency dramatically.
authors.affiliation: Biomedicinal Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Yusung, Taejeon 305-706, South Korea.
authors.forename: Hyae-Gyeong
authors.initials: HG
authors.lastname: Cheon
authors.forename: Chul-Min
authors.initials: CM
authors.lastname: Lee
authors.forename: Beom-Tae
authors.initials: BT
authors.lastname: Kim
authors.forename: Ki-Jun
authors.initials: KJ
authors.lastname: Hwang
mesh_terms: D000818:Animals; D001331:Automation; D018819:Dipeptidyl Peptidase 4 / Q000187:drug effects*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D040081:Protein Array Analysis; D011810:Quinoxalines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D011480:Protease Inhibitors; D011810:Quinoxalines; D018819:Dipeptidyl Peptidase 4