| 摘要 |
Provided are pharmaceutical formulations, and methods of inhibiting fungal and parasitic activity using a compound of formula I: <IMAGE> I wherein: Rz1 is hydrogen, -CH2OH, -CHOHCH3 or -CHOHCH2C(O)NH2; Rz2 is hydrogen, -CH2OH or -CHOHCH3; Rz3 is hydrogen or methyl; Rx1 is hydrogen, hydroxy or O-Rx1'; Rx1' is C1-C6 alkyl, benzyl, -(CH2)2Si(CH3)3, -CH2CH=CH2, -CH2CHOHCH2OH, -(CH2)aCOOH, -(CH2)bNRw1Rw2, -(CH2)cPORw3Rw4 or -[(CH2)2O]d-(C1-C6)alkyl; a, b and c are independently 1, 2, 3, 4, 5 or 6; Rw1 and Rw2 are independently hydrogen, C1-C6 alkyl, or Rw1 and Rw2 combine to form -CH2(CH2)eCH2-; Rw3 and Rw4 are independently hydroxy, or C1-C6 alkoxy; d is 1 or 2; e is 1, 2 or 3; Rx2, Ry1, Ry2, Ry3 and Ry4 are independently hydroxy or hydrogen; R0 is hydroxy, -OP(O)(OH)2 or a group of the formulae: <IMAGE> R1 is C1-C6 alkyl, phenyl, p-halo-phenyl, p-nitrophenyl, benzyl, p-halo-benzyl or p-nitro-benzyl; R2 is <IMAGE> R3 is <IMAGE> <IMAGE> <IMAGE> or <IMAGE> R3a, R3b, R3c and R3d are independently hydrogen, C1-C12 alkyl, C2-C12 alkynyl, C1-C12 alkoxy, C1-C12 alkylthio, halo, -O-(CH2)m-[O-(CH2)n]p-O-(C1-C12 alkyl) or -O-(CH2)q-X-R4; m is 2, 3 or 4; n is 2, 3 or 4; p is 0 or 1; q is 2, 3 or 4; X is pyrrolidino, piperidino or piperazino; and R4 is hydrogen, C1-C12 alkyl, C3-C12 cycloalkyl, benzyl or C3-C12 cycloalkylmethyl; with the proviso that at least one of Rz1 and Rz2 must be hydrogen;
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