Synthesis of Novel Indole Hydrazone Derivatives and Evaluation of Their Antiplatelet Aggregation Activity
作者:Vida Mashayekhi、Kamaleddin Haj Mohammad Ebrahim Tehrani、Salimeh Amidi、Farzad Kobarfard
DOI:10.1248/cpb.c12-00597
日期:——
Based on the existing reports regarding the antiplatelet aggregation activity of hydrazone derivatives, a series of indole hydrazone derivatives were considered as potential antiplatelet agents and synthesized. The structures of the synthesized compounds were confirmed by spectral data and elemental analysis. The new indole hydrazone derivatives were evaluated for their ability to inhibit platelet aggregation induced by adenosine diphosphate (ADP) and arachidonic acid (AA). Compounds 1h and 3h exhibited remarkable activity against arachidonic acid induced platelet aggregation with IC50 values comparable to that of indomethacin and compound 1i efficiently inhibited platelet aggregation induced by both ADP and AA.
基于现有关于酰腙类化合物抗血小板聚集活性的报道,我们考虑合成一系列吲哚酰腙衍生物作为潜在的抗血小板药物。通过光谱数据和元素分析确认了合成化合物的结构。这些新型吲哚酰腙衍生物被评估了其抑制由二磷酸腺苷(ADP)和花生四烯酸(AA)诱导的血小板聚集的能力。化合物1h和3h对花生四烯酸诱导的血小板聚集表现出显著的抑制活性,其IC50值与吲哚美辛相当,而化合物1i则有效地抑制了由ADP和AA诱导的血小板聚集。