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ID: ALA3098001

Journal: Bioorg Med Chem Lett

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

Authors: Tu W, Fan J, Zhang H, Xu G, Liu Z, Qu J, Yang F, Zhang L, Luan T, Yuan J, Gong A, Feng J, Sun P, Dong Q.

Abstract: 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.

CiteXplore: 24332627

DOI: 10.1016/j.bmcl.2013.11.055