1-(9H-咔唑-4-氧)-3-取代氨基-2-丙醇类化合物的合成及生物活性(Ⅱ)

Synthesis and Bio-activity of 1-(9H-Carbazol-4-yloxy)-3-Substituted Amino-2-Propanol Compounds Ⅱ.

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 3个 1- ( 9H-咔唑 - 4-氧 ) - 3 -取代氨基 -2 -丙醇类化合物 V1 1 ～ V1 3及其 6个相应的酯化物 VI1 ～VI6 。结果和讨论 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 ,9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 2 、 3、

AIM The purpose is to make a search for new compounds with β-adrenergic recepotor antagonistic action. METHOD Using carazolol as a lead compound, the 1-(9H-carbazol-4-yloxy)-3-substituted amino-2-propanol compounds were designed and synthesized, all of which were not reported previously. Their structures were identified by IR, 1HNMR, EA or HRMS. RESULTS AND CONCLUSION The preliminary biological tests suggested that all the ten compounds could inhibit isoprenaline-induced tachycardia to different extent, and three of them showed better activity.