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(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2007 Oct 15 , DOI: 10.1016/j.bmcl.2007.07.081
Stephen W. Wright , Mark J. Ammirati , Kim M. Andrews , Anne M. Brodeur , Dennis E. Danley , Shawn D. Doran , Jay S. Lillquist , Shenping Liu , Lester D. McClure , R. Kirk McPherson , Thanh V. Olson , Stephen J. Orena , Janice C. Parker , Benjamin N. Rocke , Walter C. Soeller , Carolyn B. Soglia , Judith L. Treadway , Maria A. VanVolkenburg , Zhengrong Zhao , Eric D. Cox

A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.

中文翻译:

二肽基肽酶IV的(3R,4S)-4-(2,4,5-三氟苯基)-吡咯烷-3-基胺抑制剂:合成,体外,体内和X射线晶体学表征。

从用于治疗2型糖尿病的高通量筛选命中,开发了一系列基于吡咯烷的二肽基肽酶IV抑制剂。对效能,选择性和药代动力学特性进行了优化,从而确定了临床前候选药物,以进行进一步的分析。
更新日期:2017-01-31
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