刘超美, 杨济秋, 刘丽琳. (E)-1-芳基-2-咪唑乙酮和(E)-1-芳基-2-苯并咪唑乙酮取代苯腙衍生物的合成及其抗真菌活性J. 药学学报, 1987, 22(10): 736-745.
引用本文: 刘超美, 杨济秋, 刘丽琳. (E)-1-芳基-2-咪唑乙酮和(E)-1-芳基-2-苯并咪唑乙酮取代苯腙衍生物的合成及其抗真菌活性J. 药学学报, 1987, 22(10): 736-745.
LIU Chao-Mei, YANG Ji-Qiu , LIU Li-Lin, . STUDIES ON THE SYNTHESIS OF (E)-SUBSTITUTED PHENYLHYDRAZONES OF 1-ARYL-2-IMIDAZOLYL AND BEN ZIMIDAZOLYL ETHANONE AND THEIR ANTIFUNGAL ACTIVITYJ. Acta Pharmaceutica Sinica, 1987, 22(10): 736-745.
Citation: LIU Chao-Mei, YANG Ji-Qiu , LIU Li-Lin, . STUDIES ON THE SYNTHESIS OF (E)-SUBSTITUTED PHENYLHYDRAZONES OF 1-ARYL-2-IMIDAZOLYL AND BEN ZIMIDAZOLYL ETHANONE AND THEIR ANTIFUNGAL ACTIVITYJ. Acta Pharmaceutica Sinica, 1987, 22(10): 736-745.

(E)-1-芳基-2-咪唑乙酮和(E)-1-芳基-2-苯并咪唑乙酮取代苯腙衍生物的合成及其抗真菌活性

STUDIES ON THE SYNTHESIS OF (E)-SUBSTITUTED PHENYLHYDRAZONES OF 1-ARYL-2-IMIDAZOLYL AND BEN ZIMIDAZOLYL ETHANONE AND THEIR ANTIFUNGAL ACTIVITY

  • 摘要: 根据抗真菌药物的作用机理和构效关系,本文设计合成了61个(E)-1-芳基-2-咪唑乙酮和(E)-1-芳基-2-苯并咪唑乙酮取代苯腙衍生物,其中57个化合物是未知的。初步抑菌试验结果表明,大多数化合物对深部致病真菌具有不同程度的抑菌作用。当苯环上有2,6-Cl2,2,4-Cl2,p-Cl,p-NO2,p-OCH3,p-SCH3取代时,抗真菌活性较强,特别是有p-OCH3取代的化合物(如:13,29,45)抗真菌活性优于或相似于克霉唑,抗菌谱也较广。

     

    Abstract: In an effort to search for more potent and less toxic antimycotic agents, 61(E)-substituted phenylhydrazones of 1-aryl-2-(1H-imidazol-1-yl) ethanone and 1-aryl-2-(1H-benzimidazol-1-yl) ethanone were synthesized. Fifty seven out of 61 title compounds are first reported.The results of preliminary biological tests showed that most of the title compounds have inhibitory activity against pathogenic fungi such as Trichophyton rubrum, Trichophyton gypseum, Microsporum gypseum, Epidermophyton floccosum, Candida albicans, Cryptococcus neoformans and Cladosporium carrionii; some of them with substitution of 2,6-Cl2, 2,4-Cl2, p-NO2, p-Cl, p-CH3, p-OCH3, p-SCH3 on the phenyl ring have better inhibitory activity against fungi, especially deep pathogenetic fungi, like Candida albicans and Cryptococcus neoformans. Compounds 13, 29, 42, 45, 47 and 61 are even better than clotrimazole.

     

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