Synthesis and biological evaluation of cyclopentyl-triazolol-pyrimidine (CPTP) based P2Y12 antagonists.

Wangyang Tu,Jiang Fan,Haitang Zhang,Guoji Xu,Zhiwei Liu,Jian Qu,Fanglong Yang,Lei Zhang,Tianyu Luan,Jijun Yuan,Aishen Gong,Jun Feng,Piaoyang Sun,Qing Dong

Bioorganic & Medicinal Chemistry Letters（2014）

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摘要

In this Letter we describe SAR investigation on the cyclopentyl-triazolol-pyrimidine scaffold in pursuit of new oral P2Y12 inhibitors. Different synthetic routes were developed for variations at the cyclopentyl core. Optimization finally led to compound 2d which was advanced into preclinical development based on better potency and safety profile in comparison to ticagrelor.

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关键词

Anti-platelet,P2Y12 receptor antagonist,Ticagrelor,Excessive bleeding

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