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...

Crude enzymepreparations of Streptomyces coelicolor (Miiller), UC 5240 in the presence of ATP and Mg2+ catalyzed the conversion of oleandomycin, tylosin, leucomycin A3 and a mixture of spiramycins I, II and III to their antibiotically inactive I'-O-phosphates.10 Under identical conditions, erythromycin was converted to anhydroerythromycin-Z'-O-phosphate.10 As O-phosphorylation of aminocyclitols...

The effect of four macrolide antibiotics (roxithromycin, clarithromycin, erythromycin, and azithromycin) on the generation of some mediators and cytokines involved in the inflammatory process has been studied both in vivo and in vitro. Rat carrageenin pleurisy was used as a model of acute inflammation, and the macrolides were administered (10, 20, and 40 mg/kg p.o.) 1 h before the carrageenin c...