Novel butynyl group incorporated pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors
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.
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 M). Consequently, compound 78 (IC50= 1.55 nM) was identified to be a potent, selective, and orally available lead, worth further evaluations and optimizations.
Zhengchao Tu、Wenhui Hu、Hongjiang Xu、Xiquan Zhang、Xin Zhao、Shaogao Zeng、Xin Lu、Hui Xiea、Guicheng Zhang、Lili Zeng、Ling Yang
药学生物化学分子生物学
PP-IV inhibitortype 2 diabeteshit to lead optimization SAR study.
Zhengchao Tu,Wenhui Hu,Hongjiang Xu,Xiquan Zhang,Xin Zhao,Shaogao Zeng,Xin Lu,Hui Xiea,Guicheng Zhang,Lili Zeng,Ling Yang.Novel butynyl group incorporated pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors[EB/OL].(2017-11-17)[2025-08-02].https://chinaxiv.org/abs/201711.02420.点此复制
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