以2-乙氧羰基取代的1,5-苯并硫氮杂卓A1和A2为模型化合物,合成了3个系列34个1,5-苯并硫氮杂卓衍生物11~17,考察了它们对新生隐球菌的抑菌活性及杂卓A1和A2的构效关系。研究结果表明,杂卓A1和A2分子中2-位的乙酯基与七元杂环直接相连对其抗真菌活性是必要的。%Using 2-ethoxycarbonyl-substituted 1,5-benzothiazepines A1 and A2 as the prototy-pical structure, three series of thirty-four 1 ,5-benzothiazepine derivatives 11-17 were synthesized and evalu-ated for their an-tifungal activity against C. neoformans. The results suggested that the ethoxycarbonyl group at the position 2 of benzothiazepines A1 and A2 was essential for their antifungal activity.
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