POLYENE MAGROLIDE DERIVATIVES. II

N-glycosyl derivatives of polyene macrolide antibiotics.

Sir: The polyene macrolides are known as potent antifungal agents. However their use in therapy is limited by considerable toxicity and very poor water solubility. Many efforts had been taken to obvert these undesirable properties1-5). We report now a new group of derivatives of polyene macrolides exhibiting improved solubility in water and organic solvents and retaining the biological activity...

Methyl esters of trimethylammonium derivatives of polyene macrolide antibiotics.

A new polyene antibiotic, flavomycoin. Structural investigations. II.

Flavomycoin is a polyene antibiotic isolated from the mycelium of Streptomyces roseoflavus ARAI 1951 var. jenensis nov. var. JA 5068 as yellow-green crystals. It shows inhibitive activities against yeasts and fungi as well as protozoa. It is optically active, exhibits an ultraviolet spectrum without fine structure with maxima at 363 nm and 263 nm. Analytical studies indicated that the molecular...

A tailoring activity is responsible for generating polyene amide derivatives in Streptomyces diastaticus var. 108.

We recently characterized rimocidin B (3b) and CE-108B (4b) as two polyene amides with improved pharmacological properties, produced by genetically modified Streptomyces diastaticus var. 108. In this work, genetic and biochemical analysis of the producer strain show that the two amides are derived from the parental polyenes rimocidin (3a) and CE-108 (4a) by a post-PKS modification of the free s...

Hydrazides--a novel type of derivatives of polyene macrolide antifungal antibiotics.

properties ofpolyene macrolides wehave established the structure-activity relationship among the derivatives of amphotericin B, the polyene antibiotic most commonly used in clinical practice11}. It has been shown in these studies that the improvement of selective toxicity is related to the absence of a free carboxyl group in the modified antibiotic molecule. Wehave also demonstrated that water ...