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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-Cl_2,2,4-Cl_2,p-Cl,p-NO_2,p-OCH_3,p-SCH_3取代时,抗真菌活性较强,特别是有p-OCH_3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。
According to the mechanism of action and the structure-activity relationship of antifungal agents, 61 (E) -1-aryl-2-imidazolones and (E) -1-aryl-2-benzimidazolones were designed and synthesized Phenylhydrazone derivatives, of which 57 compounds are unknown. Preliminary antibacterial test results show that most of the compounds on the deep pathogenic fungi have different degrees of inhibition. When 2,6-Cl_2, 2, 4-Cl_2, p-Cl, p-NO_2, p-OCH_3 and p-SCH_3 are substituted on the benzene ring, the antifungal activity is strong, especially p-OCH_3 substituted compounds (Such as: 13,29,45) antifungal activity is superior to or similar to clotrimazole, antibacterial spectrum is also wider.