Method for modification of macrolide antibiotic oligomycin a by reaction of [3+2]-dipolar cycloconnection of azide and alkines 33-deoxy-33-(triazol-1-yl)-oligomycins a and their biological activity

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to the pharmaceutical industry and concerns new derivatives of the antitumour antibiotic oligomycin A and a method for preparing them by regioselective [3+2]-dipolar cycloconnection of an azido group of 33-deoxy-33-azidooligomycin A(1) to monosubstituted alkines. The new derivatives of the antibiotic oligomycin A described by formula: , wherein R represents 1,4-disubstituted 1,2,3-triazoles, namely a. - (phenyl-triazol-1-yl), b. - (4-carboxy-triazol-1-yl), c. - (4-4-methoxycarbonyl-triazol-1-yl), d. - (4-dimethylaminoethylamidocarboxytriazol-1-yl) possess manifested antitumour activity and higher solubility as compared to the initial oligomycin A. EFFECT: preparing the new derivatives of the antitumour antibiotic. 3 cl, 4 dwg, 3 tbl