The analogues of promising antitubercular compound 6-ethoxycarbonyl-7-(2-thienyl)-5-methyl-4,7-dihydro1,2,4-triazolo[1,5- a ]pyrimidine were synthesized. Variation of the CH-active, carbonyl and azole components was carried out. Tuberculostatic activity of synthesized compounds was studied and “structure-activity” dependency was analyzed.