| abstract |
Attorney Docket No. UIX-014.25 nABSTRACT nProvided are certain derivatives of amphotericin B (AmB) characterized by reduced ntoxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea nderivatives ofAmB. Certain of the derivatives are C3, C5, C8, C9, C1I, C13, or C15 n5 deoxy derivatives of AmB. Certain of the derivatives include C3'or C4' modifications of nthe mycosamine appendage of AmB. Also provided are methods of making AmB nderivatives of the invention, pharmaceutical compositions comprising AmB derivatives of nthe invention, and methods of use of AmB derivatives of the invention. n- 65-n1/33 nFigure 1 nOH OH nHO OH OH OHOHOH nHO /'MeO OH OH OH OH O,,,,16R nOR' n0 Me namphotericin B (AmB) COOH OH nOH NH 2 n0 Me namphotericin B methyl ester (AmBME) COOMe OH nOH NH 2 namphoternolide (AmdeB) COOH H n0 Me nC2'deoxy amphotericin B (C2'deOAmB) COOH OH nNH 2 |