LAUSR

Based on previous studies indicating the pharmacophoric role of a hydrazone group and azole rings for antiplatelet aggregation activity, a few series of compounds with both hydrazone and an azole (imidazole) ring in their structures were synthesized, and their platelet aggregation inhibitory effects were evaluated. Two of these 1‐(arylideneamino)‐4‐aryl‐1H‐imidazole‐2‐amine derivatives, compounds 4 a [(E)‐1‐(benzylideneamino)‐4‐phenyl‐1H‐imidazol‐2‐amine] and 4 p [(E)‐4‐phenyl‐1‐((thiophen‐2‐ylmethylene)amino)‐1H‐imidazol‐2‐amine], exhibited IC50 values similar to that of acetylsalicylic acid against collagen as a platelet aggregation inducer. Structural comparison of the synthesized compounds revealed that those with a para‐substituted phenyl ring on the imidazole were among the most active compounds against platelet aggregation induced by arachidonic acid (AA), and the presence of a thiophene ring in these compounds maximized their antiplatelet activity.