UREA DERIVATIVES OF POLYENE MACROLIDE ANTIBIOTICS

摘要

Disclosed are urea derivatives of polyene macrolide antibiotics, other than amphotericin B, comprising a urea-containing substructure represented by wherein R represents hydrogen, alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, aminoalkyl, or -(CH₂)_n-COOH; and n is 1, 2, 3, 4, 5, or 6. Also disclosed are pharmaceutical compositions comprising the urea derivatives, methods of using the urea derivatives to inhibit growth of a yeast or fungus, and methods of treating a yeast or fungal infection. In various embodiments, the polyene macrolide antibiotic is selected from the group consisting of amphotericin A, arenomycin B, candicidin D, candidin, candidoin, CE-108, etruscomycin, eurocidin D, eurocidin E, FR-008-VI, HA-2-91, hamycin A, levorin AO, levorin A3, mycoheptin, natamycin (pimaricin), nystatin Al, nystatin A2, nystatin A3, partricin A, polyfungin B, rimocidin, tetramycin A, tetramycin B, tetrin A, tetrin B, tetrin C, trichomycin A, trichomycin B, vacidin A, YS-822A, 3874 HI, 3874 H2, 3874 H3, and 67-121-A.