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根据氮唑类和烯丙胺类抗真菌化合物的构效关系、作用机理。设计合成了30个N-(6,6-二甲基-2-庚烯-4-炔基)-N-甲基-α-取代-1-(4-取代)萘甲胺类化合物。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Ⅰ_(1a)的真菌活性大致与克霉唑相当,对白念珠菌的活性明显高于naftifine和terbinafine,但对其它七种菌株的活性均不及naftifine和terbinafine;化合物Ⅲ_(1a)对八种试验菌株的活性均与terbinafine相当。
According to the structure-activity relationship between azoles and allylamine antifungal compounds, the mechanism of action. Thirty N- (6,6-dimethyl-2-hepten-4-ynyl) -N-methyl-α-substituted 1- (4-substituted) naphthalenemethylamine compounds were designed and synthesized. 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 compound Ⅰ_ (1a) was almost the same as that of clotrimazole. The activity of Candida albicans was significantly higher than that of naftifine and terbinafine, but none of the other seven strains were as good as naftifine and terbinafine. Compound Ⅲ_ (1a) Strain activity are comparable with terbinafine.