A series of novel thienopyridine derivatives were designed and synthesized as P2Y₁₂ receptor inhibitors. Several solid compounds were assessed for inhibitory effect where they exhibited stronger potency than clopidogrel. Compound 6b and 6g were evaluated for metabolism to verify that they could overcome clopidogrel resistance and for toxicity where they showed lower toxicity than prasugrel. Compound 6b exhibited lower risk of bleeding than prasugrel and showed good stability under stress testing. Overall, as a promising antiplatelet agent, representative compound 6b showed the following advantages: (1) no drug resistance for CYP2C19 poor metabolizers; (2) higher potency than clopidogrel; (3) lower toxicity than prasugrel; (4) lower risk of bleeding than prasugrel; (5) good stability as a non-salt solid.

设计并合成了一系列新型噻吩并吡啶衍生物作为P2Y ₁₂受体抑制剂。评估了几种固体化合物的抑制作用，它们表现出比氯吡格雷更强的效力。对化合物6b和6g的代谢进行了评估，以验证它们可以克服氯吡格雷抗性和毒性，其中它们显示出比普拉格雷更低的毒性。与普拉格雷相比，化合物6b表现出较低的出血风险，并且在压力测试下表现出良好的稳定性。总体而言，作为一种有前途的抗血小板药物，代表化合物6b表现出以下优点：（1）对CYP2C19弱代谢者无耐药性；(2) 比氯吡格雷效力更高；(3) 毒性低于普拉格雷；(4) 出血风险低于普拉格雷；(5)作为非盐固体具有良好的稳定性。