苯丙烯酰胺类化合物的设计、合成及抗血小板聚集活性

Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation

依据拼合原理,设计并合成了20个具有苯丙烯酰胺类结构的化合物,其结构均经IR、~1H NMR、^(13)C NMR和MS确证。采用Bron比浊法测定了所有化合物对二磷酸腺苷(adenosine diphoshate,ADP)及花生四烯酸(arachidonic acid,AA)诱导的血小板聚集的抑制活性。初步药理结果显示,化合物6b、9b、9d和9h对AA诱导的血小板聚集具有较好的抑制作用;化合物6b、6d、6j、9b和9g对ADP诱导的血小板聚集具有较好的抑制作用。

Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-eombination strategy. The structures of target compounds were elucidated by IR, ^1HNMR, ^13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate （ADP） and （AA） arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.