Distamycin a derivatives as anti-malarial agents

Compounds of general formula (I) ##STR34## and pharmaceutically acceptable salts thereof wherein:

• n is 0 or an integer comprised between 1 and 4;
• R is selected from the group consisting of H, --OR.sub.2, or --NR.sub.3 R.sub.4 wherein:
• R.sub.2 is selected from the group consisting of H, methyl, ethyl, isopropyl, butyl, cyclopropyl, cyclopentyl, cyclohexyl, phenyl or benzyl;
• R.sub.3 and R.sub.4, independently from each other, are selected from the group consisting of H, methyl, ethyl, isopropyl, butyl, cyclopentyl, cyclopropyl, cyclohexyl or a benzyl group, phenyl, pyrrol, 1-methylpyrrol, thiophene, furan, thiazole, pyridine or imidazole, optionally substituted by a formamido or carbamoyl-group or, when taken together, from a group selected from propylene, butylene, --(CH.sub.2).sub.2 --O--(CH.sub.2) .sub.2 -- or --(CH.sub.2)--NH--(CH.sub.2).sub.2 --;
• R.sub.1 is selected from the group consisting of:
• ##STR35## --COOR.sub.5, wherein R.sub.5 is selected from the group consisting of H, methyl, ethyl, isopropyl, butyl, cyclopropyl, cyclopentyl, cyclohexyl, benzyl, phenyl or a cholesterol type group;
• --B--NR.sub.6 R.sub.7 wherein B is selected from the group consisting of a simple chemical bond and the group C.dbd.O and wherein R.sub.6 and R.sub.7, independently from each other, are selected from the group consisting of H, methyl, ethyl, isopropyl, butyl, cyclopropyl, cyclopentyl, cyclohexyl, benzyl or phenyl, or, taken together, form a group selected from propylene, butylene, --(CH.sub.2).sub.2 --O--(CH.sub.2) .sub.2 -- or --(CH.sub.2).sub.2 --NH--(CH.sub.2).sub.2 --;
• a heterocyclic group selected from ##STR36## A is a simple chemical bond or the group CO--NH--Z wherein Z is a methylene-, ethylene-, propylene- or p-phenylene group
• with the proviso that:
• when R.sub.1 is --B--NR.sub.6 R.sub.7 and B is a simple chemical bond, A is not a simple chemical bond;
• when R.sub.1 is one of the above indicated heterocyclic groups, A is not a simple chemical bond;
• when R is NH.sub.2, A is the group CO--NH--Z, wherein Z is --CH.sub.2 --CH.sub.2 and R.sub.1 is ##STR37## then n is different from 1;
• when R is the group NH.sub.2, R.sub.1 is --COOH and A is a simple chemical bond, then n is different from 0;
• when R is OH, R.sub.1 is ##STR38## and A is the group --CO--NH--Z, then Z is different from --CH.sub.2 --CH.sub.2.