Structural Variations Beyond itraconazole:Discovery of Highly Potent Antifungal Compounds for Dermat

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:wori123ri123
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  In this presentation we will present structural variations of itraconazole with the aim to improve its activity against dermatomycosis and systemic fungal infections.The most potent compounds were compared in vitro and in vivo against terbinafine and voriconazole for dermatomycosis and Aspergillus infections,respectively.In the search for new compounds with potential for clinical use as antifungal agents in dermatology,our compound database was scanned for azole compounds with excellent activity against experimental dermatophytosis in vivo,regardless of anti-Candida activity.A top three compounds was chosen as lead compounds and twelve different combinations of the enantiomerical pure dioxolane precursors and the phenol backbones were synthesized.The presention summarizes the findings with these new azoles in tests for antifungal activity in vitro and in animal models for superficial mycoses.These results led to the discovery of pramiconazole.
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