Pradimicin derivatives.

摘要

The present invention provides pradimicin analogs of formula (II) which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections. <CHEM> wherein R<1> is selected from the group consisting of H, methyl, and hydroxymethyl, and when R<1> is methyl or hydroxymethyl, the resulting amino acid has the D-configuration; R<2> is H or beta -D-xylosyl; R<3> is H or methyl; and R<4> is selected from the group consisting of (C2-5)alkenyl; (C2-5)alkynyl; substituted (C1-5)alkyl; substituted (C2-5)alkenyl; wherein the substituent for both the alkyl and alkenyl is a group selected from the group consisting of, carboxy, (C1-5)alkoxycarbonyl, carbamyl, (C1-5)alkylcarbamyl, di(C1-5)alkylcarbamyl, and sulfonyl; (C1-5)alkanoyl substituted with a group selected from the group consisting of amino, (C1-5)alkylamino, and di(C1-5)alkylamino; L-glutamyl; formyl; benzyl; and p-tolylsulfonylcarbamyl; or a pharmaceutically acceptable salt thereof.