SELECTIVE ANTITUBERCULOUS AGENTS REPRESENTING SUBSTITUTED 7-ARYL(HETERYL)-6-CARBETHOXY-4,7-DIHYDRO-1,2,4-TRIAZOLE[1,5-a]PYRIMIDINES OR SUBSTITUTED 7-ARYL(HETERYL)-4,7-DIHYDRO-6-NITRO-1,2,4-TRIAZOLE[1,5-a]PYRIMIDINES OR THEIR PHARMACEUTICALLY ACCEPTABLE ADDITIVE SALTS, PHARMACEUTICAL COMPOSITION THEREOF AND METHOD FOR PREPARATION OF SUBSTITUTED 7-ARYL(HETERYL)-6-CARBETHOXY-5-METHYL-4,7-DIHYDRO-1,2,4-TRIAZOLE[1,5-a]PYRIMIDINES Russian patent published in 2009 - IPC C07D239/70 C07D487/04 A61K31/519 A61P31/06 

FIELD: chemistry, medicine.

SUBSTANCE: selective antituberculous agents represent substituted 7-aryl(heteryl)-4,7-dihydro-1,2,4-triazole/1,5-a/pyrimidines of general formula A or B or their pharmaceutically acceptable additive sodium or potassium salts of the compound B, where in the formula A R₁ = hydrogen atom; R₂= aryl selected from the possibly substituted phenyl or heteryl selected from the thienyl, pyridyl, indolyl, pyrrolyl with substituted phenyl having 1-3 substituting groups selected from the group including methoxy-, nitro- and hydroxyl- groups; in the formula B R₁ = hydrogen atom, C₁-C₁₂ alkyl or C₁-C₁₂ thioalkyl; R₂ = aryl selected from the possibly substituted phenyl or heteryl selected from the thienyl, pyridyl, indolyl, pyrrolyl with substituted phenyl having 1-3 substituting groups selected from the group including methylenedioxy-, hydroxyl-, bromine, C₁-C₆ alkyl and C₁-C₆ alkoxy groups and substituted heteryl having substituting group selected from bromine, C₁-C₆ alkoxy and C₁-C₆ alkyl groups. The invention refers also to the method for preparation of the compounds with general formula A including the heating of the equimolar amounts of aryl- or heteroarylaldehyde, acetoacetic ester and aminotriazole in the aliphatic alcohol under ultrasonic action and to the pharmaceutical composition.

EFFECT: in comparison with the analogues the claimed agents possess higher activity and lower toxicity.

4 cl, 8 tbl, 18 ex