Lead discovery of quinoxalinediones as an inhibitor of dipeptidyl peptidase-IV (DPP-IV) by high-throughput screening.
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.
Cheon
Hyae-Gyeong
HG
Biomedicinal Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Yusung, Taejeon 305-706, South Korea.
Lee
Chul-Min
CM
Kim
Beom-Tae
BT
Hwang
Ki-Jun
KJ
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
D011480:Protease Inhibitors; D011810:Quinoxalines; D018819:Dipeptidyl Peptidase 4