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、体内及X射线晶体学表征
(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.
作者信息
Wright Stephen W, Ammirati Mark J, Andrews Kim M, Brodeur Anne M, Danley Dennis E, Doran Shawn D, Lillquist Jay S, Liu Shenping, McClure Lester D, McPherson R Kirk, Olson Thanh V, Orena Stephen J, Parker Janice C, Rocke Benjamin N, Soeller Walter C, Soglia Carolyn B, Treadway Judith L, Vanvolkenburg Maria A, Zhao Zhengrong, Cox Eric D
机构信息
Pfizer Global Research and Development, Cardiovascular and Metabolic Diseases, MS 8220-3141, Eastern Point Road, Groton, CT 06340, USA.
出版信息
Bioorg Med Chem Lett. 2007 Oct 15;17(20):5638-42. doi: 10.1016/j.bmcl.2007.07.081. Epub 2007 Aug 22.
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.
从用于治疗2型糖尿病的高通量筛选命中物出发，开发了一系列基于吡咯烷的二肽基肽酶IV抑制剂。对效力、选择性和药代动力学性质进行了优化，从而鉴定出一个用于进一步分析的临床前候选物。
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