Nystatin derivatives and their use as antifungal agents

摘要

A compound that is a nystatin derivative that has an additional double bond present between C28 and C29 and that is further modified with respect to nystatin at C16 and optionally one or more of positions C5, C9, C10 or at the amino group of mycosamine , having the formula (I) ** Formula ** in which, R1 and R2 each independently represent a hydrogen atom, a hydroxyl group, an alkoxy group, an acyloxy group or an alkyl group, or together they form a carbonyl group; R3 and R4 each independently represent a hydrogen atom, a hydroxyl group, an alkoxy group, an acyloxy group, or an alkyl group, or together form a carbonyl group; R5 and R6 each independently represent a hydrogen atom, a hydroxyl group, an alkoxy group, an acyloxy group or an alkyl group; R7 represents an alkyl group or an amide group; R8 and R9 each independently represent a hydrogen atom, an alkylamino group, a sugar group or an acyl group; or a pharmaceutically acceptable salt thereof, wherein "alkyl group" means a branched or straight chain, cyclic or acyclic saturated hydrocarbon group, containing up to 20 carbon atoms, which may be unsubstituted or substituted by a substituent selected from the hydroxy, alkoxy, acyloxy and amino groups, and which may be interrupted by one or more groups selected from -aryl-, -O-, -NR12- and -S-, in which R12 represents an atom of hydrogen or a C1-6 alkyl group; by "alkoxy group" is meant a group -OR, where R is an alkyl group as defined herein above; by "acyloxy group" is meant a -OCOR14 group, wherein R14 is an alkyl group as defined herein above; by "alkylamino group" is meant a group - (CH2) xNR16R17 where x is 1 to 10 and R16 and R17 each independently represent a hydrogen atom or a C1-6 alkyl group; by "sugar group" is meant a saccharide, preferably an oligo- or monosaccharide; by "acyl group" is meant a group -COR18 where R18 is an alkyl group as defined above; By "amide group" is meant a group of formula (III): ** Formula ** in which R10 and R11 each independently represent a hydrogen atom or an optionally substituted alkyl group as defined herein above, or together they form an alkyl ring.