.4 - Chromanone Derivatives And Analogues And Anti-platelet Aggregation Activity

4-chromanones and 4-chromones are known to exihibit a wide range of biological activities. Mannich bases at 3-position of 4-chromanones synthesized in our laboratory exhibit the significant anti-platelet aggregative activity. In this paper, the classification, mechanisms of action and advance of anti-platelet aggregative drugs are summarized, and the anti-platelet aggregative activity of 4-chromanones and 4-chromones is introduced.On the base of our previous work, 3-position substituted 4-chromanones, 3-position substituted 4-chromones, Mannich bases at aromatic ring of 4-chromanones and 4-chromones are designed as the candidates of platelet aggregative inhibitors. 18 target compounds were synthesized and characterized by 1H-NMR, IR, LC-MS and GC-MS, among which 13 compounds were not reported in the literature.Using Bern's method the anti-platelet aggregative activity of the target compounds was tested. According to screening results, some of the target compounds such as PL 17 and PL 19 showed potent inhibitory activity against rabbit platelet aggregation induced by ADP in vitro, some of the target compounds such as PL15, PL16, and PL22 showed potent inhibitory activity against rabbit platelet aggregation induced by collagen in vitro. The target compounds with anti-platelet aggregative activity in vitro need screening the inhibitory activity in vivo. To assess the relationship of the structure of 4-chromanones and 4-chromones and the inhibitory activity, some intermediates for the preparation of target compounds were tested also.Some of the structures and anti-platelet aggregative activity relationships of target compounds were surveyed.