abstract |
A cyclohexapeptide compound of general formula (I), wherein R1 is C1-C20 alkyl; C9-C20 alkenyl; C9-C20 alkoxyphenyl; an aryl group selected from: phenyl, biphenyl, terphenyl and naphthyl; C1-C12 alkylphenyl, C2-C12 alkenylphenyl, C1-C12 alkoxyphenyl; linoleoyl; palmitoyl; 12-methylmyristoyl; 10,12-dimethylmyristoyl; or -COC6H4(p)OC8H17, R1 and R3 are independently -OH; -CN; -CH2NH2; -N3; aryl; substituted aryl; heterocyclyl and substituted heterocyclic with 1-3 of the same or different heteroatoms; aminoalkylamino; mono or di-substituted linear or cyclic aminoalkylamino; -OR, wherein, R is C1-C12 alkyl; substituted alkyl of the type -(CH2)n-X, where n is 1-5 and X is Cl, Br, I, COOY, CN, NH2 or a heterocyclic and where Y is C1-C6 linear or branched alkyl; C2-C12-alkenyl; aryl; fused aryl; substituted aryl; a heterocyclic containing 1-3 heteroatoms; mono or di-substituted aminoalkyl; or a hydroxy protecting group; and R3 may additionally be imidazolyl; R2 and R4 are independently -H or -OH; R5 is -H or -CH3. R6 is -H, -CH3 or -CH2CONH2. R7 is -H, -CH3 or -OH. R8 and R9 are independently -H or -CH2-Sec.amine in which the sec.amine is attached to -CH2 through its N linkage; and its pharmaceutically acceptable salts. The compounds are useful as antifungal agents. |