1-{2-[(4-取代苯基)甲氧基]-2-(取代苯基)乙基}-1H-氮唑类化合物的合成及抗真菌活性

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。

SYNTHESIS AND ANTIFUNGAL ACTIVITY OF 1-(2-[-(4-SUBSTITUTED-PHENYL) METHOXY]-2-(SUBSTITUTED-PHENYL) ETHYL}-1H-AZOLES

Twenty nine 1-{2-1-(4-substituted-phenyl) methoxy]-2-(substituted-phenyl) ethyl}-lH-azoles were synthesized for searching of more potent and less toxic antimycotic agents. Nine of the title compounds are first reported.Results of preliminary biological tests showed that most of the title compounds exhibited activity against the common pathogenic fungi such as Candida albicans, Microsporum bodin, Trichophyton gypsum, Epidermophyton floccosum, Trichophyton violaceum, Microsporum ferrugincum, Trichophyton rubrum and Microsporum gypsum. The antifungal activity of compound 14 was roughly comparable to clotrimazole and econazole against Candida albicans, but was more active against other test fungi than clotrimazole and econazole. Compounds 4, 5, 6, 12, 23 also have good antifungal activity, but are less active against Candida albicans.