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根据氮唑类抗真菌化合物的构效关系和作用机理,设计合成了29个1-{2-[(4-取代苯基)甲氧基]-2-(取代苯基)乙基}-1H-氮唑类化合物,其中九个为首次报道。初步体外抑菌试验结果表明,大多数目标化合物对八种试验菌株都有不同程度的抗真菌活性。化合物14对白念珠菌的活性与克霉唑及益康唑相当,对其它七种试验菌株的活性明显强于克霉唑及益康唑。化合物4,12对白念珠菌活性差,对其它七种试验菌株的活性也强于克霉唑和益康唑。化合物5,6和23除对白念珠菌外,对其它七种试验菌株,也有较强活性。
According to the structure-activity relationship and mechanism of the azole antifungal compounds, 29 compounds of 1- {2 - [(4-substituted phenyl) methoxy] -2- - Azoles, nine of which were first reported. The preliminary in vitro bacteriostasis test results showed that most of the target compounds had different degrees of antifungal activity against the eight tested strains. The activity of Candida albicans against Candida albicans was comparable to that of clotrimazole and econazole, and its activity was significantly stronger than that of clotrimazole and econazole against the other seven tested strains. Candida albicans compounds 4 and 12 showed poor activity against the other seven tested strains but also clotrimazole and econazole. In addition to Candida albicans, compounds 5, 6 and 23 also showed strong activity against the other seven tested strains.