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 Russian patent published in 2014 - IPC C07D493/20 A61K31/357 A61P35/00 

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