POLYENE MACROLIDE DERIVATIVES. I

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.

The polyene macrolide antibiotics.

The mode of action of the polyene antibiotics is reviewed together with the effect of genetic and environmental factors on sensitive organisms. The future prospects of polyenes in the treatment of systemic mycoses are considered.

Trichomycin B, a polyene macrolide from Streptomyces.

Two polyene macrolide, trichomycins A and B, were compared by physico-chemical and microbiological methods. The two antibiotics were found to have the same molecular formula, C58H84N2O18 (MW 1,096), by elemental analysis and FAB-MS. However, 1H and 13C NMR spectrometry studies indicated that the hydroxyl at C-5 of trichomycin A located on C-9 in trichomycin B. Trichomycin B possessed lower acti...

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 ...