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目的 :寻找高效、低毒、生物活性更为广泛的抗心衰药物。方法 :受临床联合用药的启发 ,根据药物设计中的生物电子等排原理和结构拼合原理 ,将具有强心活性的 1 [2 (3,4 二甲氧基 )苯基 ]乙基 5 氰基 6 甲基脲嘧啶与 β 受体阻滞剂中常见的芳氧丙醇胺结构中的丙醇胺片段进行拼合 ,设计并合成了 10个 1 { 1 [2 (3,4 二甲氧基 )苯基 ]乙基 5 氰基 6 甲基脲嘧啶 3 } 3 取代氨基 2 丙醇类化合物 ,V1～ 10 。结果与结论 :所合成的目标化合物均未见文献报道 ,结构经红外光谱、核磁共振氢谱、质谱和元素分析确证。初步药理筛选结果显示 ,大部分目标化合物有不同程度的强心活性 ,Ⅴ9的活性较好。
Objective: To find a more effective, low toxicity, more biological activity of anti-heart failure drugs. Methods: Inspired by clinical combination therapy, 1 [2 (3,4-dimethoxy) phenyl] ethyl 5 cyano group with cardiotonicity was synthesized according to the principle of bioisosterism in drug design and the principle of structural assembly 6 methyluracil and beta blockers in a common structure of aryloxypropanolamine propanolamine fragments were combined to design and synthesis of 10 1 {1 [2 (3,4-dimethoxy) Phenyl] ethyl 5 cyano 6 methyl uracil 3} 3 substituted amino 2 propanol compounds, V1 ~ 10. RESULTS AND CONCLUSION: None of the synthesized target compounds were reported in the literature. The structures were confirmed by IR, 1H-NMR, MS and elemental analysis. Preliminary pharmacological screening results show that most of the target compounds have different levels of cardiac activity, V9 activity is better.