Chromone Derivatives And Analogues And Anti-platelet Aggregation Activity

Chromones and 4-chromanones are known to exhibit a wide range of biological activities. Mannich bases at 3-position of 4-chromanones and 6, 8-position of chromones and 4-chromanones synthesized in our laboratory exhibit the significant anti-platelet aggregative activity. In this paper, the classification, mechanisms of action and development of anti-platelet aggregative drugs were summarized, and the anti-platelet aggregative activity of chromones and 4-chromanones was introduced.On the base of our previous work, 6 or 7-aminoalkyloxychromones, 6 or 7-aminoalkyloxychromanones, 6 or 7-amidoalkyl-4-chromones and 6 or 7-amidoalkylchromanones were designed as the candidates of platelet aggregative inhibitors. 14 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 Born's method the anti-platelet aggregative activity of the target compounds was tested. Some of the target compounds such as ZH-06, ZH-12 and ZH-14 showed potent inhibitory activity against rabbit platelet aggregation induced by AA in vitro, which are considered to be tested in vivo. To assess their inhibitory activity and structure relationship of chromones and 4-chromanones, some intermediates were tested too.The structures and anti-platelet aggregative activity relationships of target compounds were surveyed.