The study of the antimicrobial activity of the derivatives of 6-(1,2,4-oxadizol-3-yl)- and 6-(2-aminothiazol-4-yl)thieno[2,3-d]pyrimidin-4-ones by the double dilution method

Abstract

Aim. To study profoundly the antimicrobial activity of the derivatives of 6-(1,2,4-oxadizol-3-yl)- and 6-(2-aminothiazol-4-yl)thieno[2,3-d]pyrimidin-4-ones by the double dilution method. Results and discussion. For the derivatives of 6-heterylthieno[2,3-d]pyrimidines, namely the derivatives of 6-(1,2,4-oxadizol-3-yl)- and 6-(2-aminothiazol-4-yl)thieno[2,3-d]pyrimidin-4-ones selected after the prescreening by the agar well diffusion method, the further antimicrobial activity study using the double dilution method was performed. The minimal bacteriostatic and bactericidal concentrations were determined. Experimental part. The synthesis of the target molecules was performed according to the methods previously developed. The antimicrobial activity was studied using the double-dilution method. Conclusions. The derivatives of 5-methyl-6-(3-aryl-1,2,4-oxadizol-5-yl)thieno[2,3-d]pyrimidin-4(3H)-one with the free position 3 of the thieno[2,3-d]pyrimidine system showed the highest bactericidal activity in the concentration of 125 μg/mL against the test-strains of S. aureus, E. coli and B. subtilis.

Keywords

• thiophene
• pyrimidine
• antibacterials