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4-色满酮类化合物和色酮类化合物具有广泛的生物活性。笔者曾发现4-色满酮3位Mannich碱类化合物具有显著的抗血小板聚集活性,为了考察在4-色满酮的3-位Mannich碱类化合物中3-位胺甲基侧链是否为加强活性的必需基团,为确定其药效构象提供信息,笔者设计合成了4种4-色满酮芳环Mannich碱类化合物,同时又合成了3种色酮芳环Mannich碱类化合物。所合成的目标化合物均未见文献报道,其组成和结构经红外光谱、质谱和核磁共振氢谱确认。采用Born’s比浊法对目标化合物进行了抗血小板聚集活性的体外筛选。实验结果表明,目标化合物对ADP和胶原诱导的家兔血小板聚集均具有显著的体外抑制活性。
4-Chromanones and Chromone compounds have a wide range of biological activities. The authors have found that 4-chromonone Mannich 3 base compounds have significant anti-platelet aggregation activity, in order to examine the 3-position Mannich base in 4-chromonaton 3-position aminomethyl side chain is enhanced In order to provide information for determining its pharmacodynamic conformation, we designed and synthesized four kinds of Mannich base compounds with 4-chromonone aromatic ring and 3 kinds of chromonuclear aromatic ring Mannich base compounds. None of the synthesized target compounds were reported in the literature, and their compositions and structures were confirmed by IR, MS and 1H-NMR. The target compounds were screened for anti-platelet aggregation activity using Born’s nephelometry. The experimental results show that the target compounds have significant in vitro inhibitory activity on ADP and collagen-induced platelet aggregation in rabbits.