【摘要】 目的合成西贝素衍生物并进行初步药理活性研究。方法采用酰化、烷基化方法合成衍生物;药理学实验在豚鼠离体气管模型上进行。结果合成4个西贝素衍生物,分别为3β-戊酰西贝素(1)、3β-异丁酰西贝素(2)、3β-乙基西贝素(3)、3β-丙基西贝素(4);观察到西贝素及其衍生物对豚鼠离体气管条平滑肌有不同程度的舒张作用。结论应用波谱法鉴定了所合成衍生物的结构,由药理学试验结果推测西贝素对气管的舒张作用并非通过M2受体调节途径,可能存在其他作用途径。更多还原

【Abstract】 OBJECTIVE To design and synthesize the imperialine’s derivatives and determine the pharmacological activities.METHODS Alkylation and acylation were used to synthesize the derivatives and the pharmacological experiments were carried out with the isolated trachea in guinea pig.RESULTS Four title compounds:3β-pentyoxyimperialine(1),3β-iso-butyoimperialine(2),3β-ethylimperialine(3) and 3β-propylimperialine(4) were synthesized and all of them could relax the guinea pig’s isolated trachea.CONCLUSION The structures of the compounds were identified by spectral data.Imperialine and its derivatives relax the guinea pig’s isolated trachea not to depend on M2 receptor as reported before,which implied the other way might exist.更多还原