李科, 张万年, 杨济秋, 吕加国, 吴秋业. 1-{2-(取代苯基)甲氧基-2-(取代苯基)乙基}-1H-三唑和苯并三唑类化合物的合成及抗真菌活性J. 药学学报, 1995, 30(3): 191-198.
引用本文: 李科, 张万年, 杨济秋, 吕加国, 吴秋业. 1-{2-(取代苯基)甲氧基-2-(取代苯基)乙基}-1H-三唑和苯并三唑类化合物的合成及抗真菌活性J. 药学学报, 1995, 30(3): 191-198.
K Li, WN zhang, JQ Yang, JG Lu , QY Wu, . SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF 1-2- (SUBSTITUTED-PHENYL)METHOXY-2-(SUDSTITUTED-PHENYL) ETHYL-1H-TRIAZOLES AND BENZTRIAZOLESJ. Acta Pharmaceutica Sinica, 1995, 30(3): 191-198.
Citation: K Li, WN zhang, JQ Yang, JG Lu , QY Wu, . SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF 1-2- (SUBSTITUTED-PHENYL)METHOXY-2-(SUDSTITUTED-PHENYL) ETHYL-1H-TRIAZOLES AND BENZTRIAZOLESJ. Acta Pharmaceutica Sinica, 1995, 30(3): 191-198.

1-{2-(取代苯基)甲氧基-2-(取代苯基)乙基}-1H-三唑和苯并三唑类化合物的合成及抗真菌活性

SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF 1-2- (SUBSTITUTED-PHENYL)METHOXY-2-(SUDSTITUTED-PHENYL) ETHYL-1H-TRIAZOLES AND BENZTRIAZOLES

  • 摘要: 报道了39个新的1-{2-(取代苯基)甲氧基-2-(取代苯基)乙基}-1H-三唑和苯并三唑类化合物的合成与体外抑菌试验,结果表明,化合物6,13的抗真菌活性为益康唑的4~10倍,化合物10,12,14,15,20,22,23,28.30和31等对大部分真菌活性也优于或相当于益康唑及克霉唑,化合物23和31抗裴氏着色菌活性为益康唑、克霉唑的30倍以上,化合物22抗白念珠菌活性为益康唑的8倍,克霉唑的4倍。

     

    Abstract: Thirty-nine1-{2-(2,4-dichlorophenyl )methoxy-2-(substituted-phenyl)ethyl}-1H-triazoles and benztriazoles were svnthesized and all title compounds are reported for the first time.Results of preliminary biological tests showed that the most active compounds 6 and 13 are 4~10times more active than the lead compound econazole.The antifungal activities of compounds 10 ,12,14,15,20,22,23,28,30 and 31 are better than or comparable to the activities of econazole andclotrimazole against most fungi.Compounds 23 and 31 are 30 times more active than econazole andclotrimazole against Fonseaea pedrosoi.Compound 22 is 4 and 8 times more active than clotrimazole andeconazole, respectively,against Candide albicans.

     

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