Synthesis and antifungal properties of papulacandin derivatives.
作者： Marjolein van der Kaaden , Eefjan Breukink , Roland J Pieters
DOI: 10.3762/BJOC.8.82
关键词:
摘要: Derivatives of an antifungal agent that targets the β-(1,3)-D-glucan synthase, papulacandin D, were synthesized and tested for activity. The D structure contains a challenging benzannulated spiroketal unit, which is introduced in palladium-catalyzed cross-coupling reaction glycal silanolate aryl iodide followed by oxidative spiroketalization. Four different variants made, differing nature acyl side chain with respect to length, number stereochemistry double bonds. Moderate biological activity was observed derivatives based on palmitic acid linoleic acid.
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