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Bioorg Med Chem Lett. 2004 May 17;14(10):2661-4.

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

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  • 1Biomedicinal Science Division, Korea Research Institute of Chemical Technology, PO Box 107, Yusung, Taejeon 305-706, South Korea.


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.

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