CYCLIC PEPTIDE ANTIFUNGAL AGENTS

摘要

Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula (I), wherein R' is hydrogen, methyl or -CH2C(0)NH2; R'' and R''' are independently hydrogen or methyl; R<x1> is C1-C6 alkyl, benzyl, -(CH2)2Si(CH3)3, -CH2CH=CH2, -CH2CHOHCH2OH, -(CH2)aCOOH, -(CH2)bNR<z1>R<z2>, -(CH2)cPOR<z3>R<z4> or -[(CH2)2O]d-(C1-C6)alkyl; a, b and c are indenpendently 1, 2, 3, 4, 5 or 6; R<z1> and R<z2> are independently hydrogen, C1-C6 alkyl, or R<z1> and R<z2> combine to form -CH2(CH2)eCH2-; R<z3> and R<z4> are independently hydroxy, or C1-C6 alkoxy; d is 1 or 2; e is 1, 2 or 3; R<x2>, R<y1>, R<y2>, R<y3> and R<y4> are independently hydroxy or hydrogen; R0 is hydroxy, -OP(0) (OH)2 or a group of formulae (a) or (b); R1 is C1-C6 alkyl, phenyl, p-halo-phenyl, p-nitrophenyl, benzyl, p-halo-benzyl or p-nitro-benzyl; and R2 is an acyl side chain as defined herein.