Sulfone II was synthesized via oxidation of ethyl 2-[5-bromo-2,4-dihydro-3-oxo-2-(thietanyl-3)-1,2,4-triazolyl- 4]acetate (I) by H₂O₂. Hydrolysis of esters I and II synthesized 2-[5-bromo-2,4-dihydro- 3-oxo-2-(thietanyl-3)-1,2,4-triazolyl-4]- and 2-[5-bromo-2,4-dihydro-3-oxo-2-(1,1-dioxothietanyl-3)-1,2,4- triazolyl-4]acetic acids III and IV, respectively.Water-soluble salts V and VI were prepared by reacting acids III and IV with alkali-metal hydroxides and amines. The structures of the synthesized compounds were confirmed IR and NMR spectroscopic data. The antiplatelet and anticoagulant activity of the synthesized compounds was studied in vitro based on predictions of the PASS computer program. Compounds III and VIb, which showed the absence of predicted toxic risks and were superior to the reference drug in the collagen-induced aggregation test, had the most pronounced antiplatelet activity (comparable to that of acetylsalicylic acid) in the ADP-induced aggregation test. The anticoagulant activity of the compounds was significantly inferior to that of heparin sodium. All synthesized compounds satisfied Lipinski’s rule-of-5.

砜II是通过 H ₂氧化 2-[5-bromo-2,4-dihydro-3-oxo-2-(thietanyl-3)-1,2,4-triazolyl-4] 乙酸乙酯 ( I ) 合成的氧₂。酯类I和II的水解合成 2-[5-bromo-2,4-dihydro-3-oxo-2-(thietanyl-3)-1,2,4-triazolyl-4]- 和 2-[5-bromo -2,4-dihydro-3-oxo-2-(1,1-dioxothietanyl-3)-1,2,4-triazolyl-4] 乙酸III和IV分别制备水溶性盐V和VI通过使酸III和IV反应与碱金属氢氧化物和胺。合成化合物的结构由 IR 和 NMR 光谱数据证实。基于PASS计算机程序的预测，在体外研究了合成化合物的抗血小板和抗凝活性。化合物III和VIb在胶原蛋白诱导的聚集试验中表现出没有预测的毒性风险并且优于参考药物，在 ADP 诱导的聚集试验中具有最显着的抗血小板活性（与乙酰水杨酸相当）。化合物的抗凝活性明显低于肝素钠。所有合成的化合物都满足 Lipinski 的 5 规则。