Patent ID: 6323176
Filing Date: 2001-11-27
Classification: A61K,A61P,C07K

Abstract:
A method of inhibiting fungal activity comprising administering to a host in need of such inhibition an effective amount of a compound of formula I ##STR78##whereinR is independently at each occurrence hydrogen, hydroxy, or O--Pg;R.sup.1 is hydrogen, methyl, CH.sub.2 C(O)NH.sub.2, CH.sub.2 C(O)NH--Pg;R.sup.2 and R.sup.3 are independently hydrogen or methyl;R.sup.4 is a moiety of the formula ##STR79##R.sup.5 is a moiety of the formula ##STR80##A is independently at each occurrence phen-di-yl, pyridin-di-yl, pyridazin-di-yl, pyrimidin-di-yl, pyrazin-di-yl, furan-di-yl, or thiophen-di-yl rings;X is independently at each occurrence a bond or C.ident.C;R.sup.6 is hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkynyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, halo, or --O--(CH.sub.2).sub.m --[O--(CH.sub.2).sub.n ].sub.p --(C.sub.1 -C.sub.12 alkyl), or --O--(CH.sub.2).sub.q --Z--R.sup.8 ;R.sup.7 is independently at each occurrence hydrogen, hydroxy, amino, azido, OR.sup.5, O--Pg, or NH.sub.p --Pg;R.sup.7' is CHR.sup.7 CH.sub.2 R.sup.7, CHR.sup.7 CH.sub.2 OR.sup.9, ethyl, CHR.sup.7 CO.sub.2 H, CHR.sup.7 CH.sub.2 O--Pg, or CHR.sup.7 C(O)--Pg;R.sup.7"" is hydrogen, CH.sub.2 R.sup.7, CH.sub.2 OR.sup.9, methyl, CO.sub.2 H, CH.sub.2 O--Pg, CH.sub.2 NH.sub.p --Pg, or C(O)--Pg;m, n, and q are independently 2, 3 or 4;p is 0 or 1;Z is pyrrolidin-di-yl, piperidin-di-yl, or piperazin-di-yl;R.sup.8 is hydrogen, C.sub.1 -C.sub.12 alkyl, benzyl, or substituted C.sub.3 -C.sub.12 cycloalkylmethyl;R.sup.9 is SO.sub.3 H or a moiety of the formula ##STR81##R.sup.10 is hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, phenyl, phenoxy, p-halophenyl, p-halophenoxy, p-nitrophenyl, p-nitrophenoxy, benzyl, benzyloxy, p-halobenzyl, p-halobenzyloxy, p-nitrobenzyl, or p-nitrobenzyloxy; andPg is a hydroxy, amino, amido or carboxy protecting group; with the proviso that the total number of R.sup.7 substituents that are OR.sup.5 groups does not exceed two; or a pharmaceutical salt or solvate thereof.