Lin Yuan, Qing-Ru Chu, Feng-Xin Li, Da-Kui Zhang, Ya-Xin Yu, Jing-Chang Liu
{"title":"Design, synthesis, and biological evaluation of Pamicogrel derivatives as potential antiplatelet agents.","authors":"Lin Yuan, Qing-Ru Chu, Feng-Xin Li, Da-Kui Zhang, Ya-Xin Yu, Jing-Chang Liu","doi":"10.1016/j.bmcl.2025.130185","DOIUrl":null,"url":null,"abstract":"<p><p>According to the bioisosterism principle and activity substructure splicing strategy, new pamicogrel derivatives were designed, synthesized, and evaluated for their antiplatelet aggregation activities in vitro. Bioassay results showed that compound SZ displayed superior in vitro antiplatelet aggregation activities induced by Arachidonic Acid (AA) and Collagen (COL) with the IC<sub>50</sub> values of 3.44 and 2.23 mg/mL, respectively. Compound BMPA showed apparent antiplatelet aggregation towards Adenosine Diphosphate (ADP) with a IC<sub>50</sub> value of 2.79 mg/mL. Significantly, compound K-10 exhibited the most antiplatelet aggregation activity to the aggregation of platelet induced by AA, ADP, and COL, representing a promising lead compound for further study.</p>","PeriodicalId":256,"journal":{"name":"Bioorganic & Medicinal Chemistry Letters","volume":" ","pages":"130185"},"PeriodicalIF":2.5000,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioorganic & Medicinal Chemistry Letters","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.bmcl.2025.130185","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
According to the bioisosterism principle and activity substructure splicing strategy, new pamicogrel derivatives were designed, synthesized, and evaluated for their antiplatelet aggregation activities in vitro. Bioassay results showed that compound SZ displayed superior in vitro antiplatelet aggregation activities induced by Arachidonic Acid (AA) and Collagen (COL) with the IC50 values of 3.44 and 2.23 mg/mL, respectively. Compound BMPA showed apparent antiplatelet aggregation towards Adenosine Diphosphate (ADP) with a IC50 value of 2.79 mg/mL. Significantly, compound K-10 exhibited the most antiplatelet aggregation activity to the aggregation of platelet induced by AA, ADP, and COL, representing a promising lead compound for further study.
期刊介绍：
Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
