Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents
Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents
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DOI：
10.1016/j.bmcl.2004.06.046
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发表时间：
2004-09-06
影响因子：
2.7
通讯作者：
Kim, SS
中科院分区：
文献类型：
--
作者：
Ahn, JH;Kim, HM;Kim, SS
通过非手性和手性合成方法合成了一系列P-2位含仲胺的氰基吡唑啉衍生物，并评价了它们对二肽基肽酶IV（DP-IV）的抑制作用。化合物5i显示出良好的体内功效（ED 50：4.1mg/kg;体内DP-IV抑制）。还发现化合物5i的具有（S）-构型的手性衍生物（11b）更有效。(C)2004爱思唯尔有限公司保留所有权利。
A new series of cyano-pyrazoline derivatives with a secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent. (C) 2004 Elsevier Ltd. All rights reserved.