Novel butynyl group incorporated pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors

分类： 物理学 >> 普通物理:统计和量子力学,量子信息等 提交时间： 2017-11-17

Shaogao Zeng Hui Xiea Lili Zeng Xin Lu Xin Zhao Guicheng Zhang Zhengchao Tu Hongjiang Xu Ling Yang Xiquan Zhang Wenhui Hu

摘要： A new chemical class of potent DPP-IV inhibitors has been structurally derived from our recently disclosed pyrrolopyrimidine scaffold by replacing cyanobenzyl with butynyl group. Systematic variations and structure-activity relationship studies have been conducted on the starting hit 51 (IC50= 0.46 μM). Consequently, compound 78 (IC50= 1.55 nM) was identified to be a potent, selective, and orally available lead, worth further evaluations and optimizations.

同行评议状态:待评议

 点击量 1622  下载量 882  评论