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目的 :寻找有 β-受体阻滞活性 ,且高效低毒的化合物。方法 :以 β-受体阻滞剂咔唑洛尔为先导化合物 ,根据药物设计中的结构拼合原理 ,对其丙醇胺侧链进行结构修饰 ,设计并合成了 1 0个 1 -( 9H-咔唑 -4 -氧 ) -3-取代氨基 -2 -丙醇类化合物 1 ～ 1 0 。结果和结论 :所合成的目的物均未见文献报道 ,结构经红外光谱、核磁共振氢谱、质谱、元素分析或高分辨质谱确证。初步药理筛选结果显示 ,1 0个化合物均能够不同程度地拮抗异丙肾上腺素引起的心动过速 ,其中化合物 1 、 3 、 4 的活性与先导化合物相似。
OBJECTIVE: To search for compounds with β-receptor blocker activity and high potency and low toxicity. Methods: Based on the structure - splitting principle of drug design, carbazole - yl, a β - receptor antagonist, was used as the lead compound to structurally modify the side chains of propanolamine. 10 1 - (9H- Carbazole - 4 - oxy) -3 - substituted amino - 2 - propanol compounds 1 ~ 1 0. RESULTS AND CONCLUSION: None of the synthesized target compounds was reported in the literature. The structures were confirmed by IR, 1H NMR, MS, elemental analysis or high resolution mass spectrometry. Preliminary pharmacological screening results showed that 10 compounds were able to antagonize isoproterenol-induced tachycardia to varying degrees, of which compounds 1, 3, 4 activity and lead compounds similar.