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Summary
Novelty: A novel compound, 3-methoxy-sampangine, and its analogues, which may be useful as antifungal agents, are disclosed. Compositions containing these compounds are also described. Sampangines are stated to be particularly effective against Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus.
Biology: Antifungal activity was determined by in vitro evaluation using a modified agar-well diffusion assay technique. These compounds exhibited in vitro activity against one or more fungal pathogens at potencies comparable to, and in many cases better than, amphotericin B.
Chemistry: The syntheses of these compounds are described in detail. Seven examples are given. Four compounds are specifically claimed, including 3-methoxy-sampangine.
Structure: