Lead discovery of quinoxalinediones as an inhibitor of dipeptidyl peptidase-IV (DPP-IV) by high-throughput screening

HG Cheon, CM Lee, BT Kim, KJ Hwang

Index: Cheon, Hyae-Gyeong; Lee, Chul-Min; Kim, Beom-Tae; Hwang, Ki-Jun Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 10 p. 2661 - 2664

Full Text: HTML

Citation Number: 17

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 ...