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

Hyae Gyeong Cheon; Chul Min Lee; Beom Tae Kim; Ki Jun Hwang

doi:10.1016/j.bmcl.2004.02.065

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

Hyae Gyeong Cheon
, Chul Min Lee
, Beom Tae Kim
, Ki Jun Hwang^*

^*Corresponding author for this work

Department of Bioenvironmental Chemistry

Korea Research Institute of Chemical Technology
Jeonbuk National University

Research output: Contribution to journal › Journal article › peer-review

22 Scopus citations

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.

Original language	English
Pages (from-to)	2661-2664
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2004.02.065
State	Published - 2004.05.17

Quacquarelli Symonds(QS) Subject Topics

Medicine
Engineering - Petroleum
Pharmacy & Pharmacology
Chemistry
Biological Sciences

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10.1016/j.bmcl.2004.02.065

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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.",

author = "Cheon, \{Hyae Gyeong\} and Lee, \{Chul Min\} and Kim, \{Beom Tae\} and Hwang, \{Ki Jun\}",

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AU - Cheon, Hyae Gyeong

AU - Lee, Chul Min

AU - Kim, Beom Tae

AU - Hwang, Ki Jun

PY - 2004/5/17

Y1 - 2004/5/17

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/1942502390

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DO - 10.1016/j.bmcl.2004.02.065

M3 - Journal article

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AN - SCOPUS:1942502390

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JO - Bioorganic and Medicinal Chemistry Letters

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IS - 10

ER -

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

Abstract

Quacquarelli Symonds(QS) Subject Topics

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