COMPARATIVE CHEMOTHERAPEUTIC ACTIVITIES OF HEPTAENE MACROLIDE ANTIFUNGAL ANTIBIOTICS IN EXPERIMENTAL CANDIDIASIS

Nine heptaene macrolide antifungal antibiotics, amphotericin B, azacolutin, candicidin, hamycin, heptamycin, levorin, mycoheptin, perimycin, and trichomycin were active against a systemic Candida albicans infection of mice. While all compounds exhibited similar activity when administered subcutaneously, only amphotericin B and mycoheptin showed significant activity when given orally. This high level of oral activity in mice is probably a characteristic of the group of heptaenes that contain only mycosamine as a nitrogenous moiety and thus should extend also to the candidin complex. Although amphotericin B is inactive when given orally to man, mycoheptin, candidin, or a chemically-modified heptaene might show useful therapeutic efficacy when given to man by the oral route.