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

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.