SYNTHESIS AND ANTIFUNGAL ACTIVITY OF SOME IMIDAZOLYL OXIME ETHER DERIVATIVES / 第二军医大学学报

ABSTRACT

Oxiconazole, a new broad-spectrum antifungal agent, was synthesized accordi ng to the method reported by Mixich G et al and some improvement was made in the preparation of N- (2, 4-dichlorobenzoylmethyl) imidazole, an important intermediate.In an effort to search for more effective antifungal drugs by chemical modification, several imidazolyl oxime ether derivatives were synthesized.The structures of the synthetic products were proved by elemental analysis.In vitro fungistatic tests showed that compounds Ⅰ-Ⅷ were more effective than clotri-mazole against most of the fungal strains tested and that compound Ⅲ possessed antifungal action against Aspergillus while others didn't.The structure of compound I(oxiconazole)was confirmed by UV, IR, 1H-NMR and MS.Its X-ray powder diffraction data are also provided.In a clinical trial,94.10% of the patients with tinea cruris were cured after a two-week oxiconazole treatments cure rate significantly higher than that of econazole(84.24%, P