Synthesis, anti‐platelet aggregation activity evaluation and structure–activity relationships of a series of novel purine derivatives,Journal of Heterocyclic Chemistry

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Synthesis, anti‐platelet aggregation activity evaluation and structure–activity relationships of a series of novel purine derivatives
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2020-05-04 , DOI: 10.1002/jhet.3997
Shunlai Li ₁ , Cheng Zhou ₁ , Mingwu Yu ₁ , Qiwen He ₁ , Hongguang Du ₁

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This article described how further extensive variation of the substituents on the purine scaffold of adenosine triphosphate (ATP), and the human anti‐platelet aggregation activities were modified in order to find exploitation of the structure–activity relationships (SAR). A series of novel designed 6‐alkylamino‐2‐alkylthio‐9‐hydroxyalkyl(carbalkoxy) purine derivatives were synthesized via a modification procedure, and the human anti‐platelet aggregation activities were evaluated. The SAR of these compounds were analyzed in detail, and the results of the structural requirements of the substituents to improve potency may provide a basis for the development of potent P2Y₁₂ antagonists.

中文翻译：

一系列新型嘌呤衍生物的合成，抗血小板凝集活性评估和构效关系

本文描述了三磷酸腺苷（ATP）嘌呤支架上取代基的进一步广泛变化以及人类抗血小板凝集活性如何被发现以利用结构-活性关系（SAR）。通过修饰程序合成了一系列新颖的6-烷基氨基-2-烷基硫基-9-羟烷基（碳烷氧基）嘌呤衍生物，并评估了其抗血小板聚集活性。对这些化合物的SAR进行了详细分析，并提出了取代基提高功效的结构要求的结果，可为开发有效的P2Y ₁₂拮抗剂提供基础。

更新日期：2020-05-04

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