Antifungal and anti-pneumocystis compounds, compositions containing such compounds, and methods of use

摘要

Compounds represented by the formula I (SEQ ID NO. 1) are disclosed: I as well as pharmaceutically acceptable salts and hydrates thereof. RI represents C9 to C19 alkyl, C9 to C19 alkenyl, an aryl group which includes phenyl, biphenyl, naphthyl and terphenyl or a C1 to C12 alkyl, alkylamino, dialkylamino or alkoxyaryl group. R1, R2 and R4 independently represent H or -OH. R3 represents H, -OH, -O(CH2)nNRVRVI, where RV and RVI independently represent H or C1-4 alkyl, or -O(CH2)nNRVRVIRVII+Y-, wherein RV and RVI are as defined above, RVII represents H or C1-4 alkyl, n is an integer of from 2-6 inclusive, and Y represents a counterion. R5 represents H, -CH3 or -OH; R6 represents H or -CH3; R7 represents H, -CH3, -CH2C(=O)NH2, -(CH2)2NRVRVI or -(CH2)2NRVRVIRVII+Y- with n, RV, RVI RVII and Y as defined above; and R8 represents -Cl, -Br, -I, -NO2, -N3, -(CH2)0-4NH2, -(CH2)0-4NH(C1-4 alkyl), -(CH2)0-4N(C1-4 alkyl)2, -(CH2)0-3CH(=NOH), -NHC(=O)(CH2)1-6NH2 or -NHC(=O)(CH2)1-6NHC(=NH)(CH2)0-3H. Pharmaceutical compositions and methods of use are also disclosed.