Azole Compound Design, Synthesis And Antifungal Activity

This article reviewed the development of anti-fungal agents at domestic and foreign in recent years. Representative of each kind of medicines with different mechanisms and compounds having presently been investigated with more powerful anti-fungal activity were introduced in the paper. New anti-fungal agents were urgently needed because fungus with anti-multi drugs have frequently been reported. Therefore, bifonazole Being taken as lead compound, 22 target compounds which were not reported in literatures were designed and synthesized in this paper. Their structures were confirmed by ¹H-NMR,¹³C-NMR and HMBC. Activity screening of some compounds were accomplished and the result indicated that the compounds had potential anti-fungal activity in vitro. In addition, ketoconazole being taken as lead compound, some analogues of ketoconazole were designed and some intermediates were synthesized in this paper.