Literature DB >> 24332627

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

Wangyang Tu1, Jiang Fan2, Haitang Zhang2, Guoji Xu2, Zhiwei Liu2, Jian Qu2, Fanglong Yang2, Lei Zhang2, Tianyu Luan2, Jijun Yuan2, Aishen Gong2, Jun Feng2, Piaoyang Sun2, Qing Dong2.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anti-platelet; Excessive bleeding; P2Y(12) receptor antagonist; Ticagrelor

Mesh：

Substances：

Year:  2013        PMID： 24332627     DOI： 10.1016/j.bmcl.2013.11.055

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  2 in total

1.  Modeling ligand recognition at the P2Y12 receptor in light of X-ray structural information.

Authors:  Silvia Paoletta; Davide Sabbadin; Ivar von Kügelgen; Sonja Hinz; Vsevolod Katritch; Kristina Hoffmann; Aliaa Abdelrahman; Jens Straßburger; Younis Baqi; Qiang Zhao; Raymond C Stevens; Stefano Moro; Christa E Müller; Kenneth A Jacobson
Journal:  J Comput Aided Mol Des       Date:  2015-07-21       Impact factor: 3.686

2.  Synthesis and biological evaluation of N 6 derivatives of 8-azapurine as novel antiplatelet agents.

Authors:  Zhichang Zhao; Yeming Wang; Nana Tian; Hong Yan; Juan Wang
Journal:  RSC Med Chem       Date:  2021-07-13
  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.