| Popis: |
A preparatively convenient one-pot method for the synthesis of new 7-thioxo[1,3]thiazolo[3,2-c]pyrimidine derivatives 3a���3l by the cyclocondensation of 5-methyl(1,3-thiazolidin-2-ylidene)ketones 1a���1c with aroyl 2a���2d and 2-thienyl 2e isothiocyanates for 6���10 h boiling in acetone has been developed. Studies of the antimicrobial and antioxidant activities potential of the obtained compounds revealed that [2-methyl-5-(4-nitrophenyl)-7-thioxo-2,3-dihydro-7H-[1,3]thiazolo[3,2-c]pyrimidine-8-yl](phenyl)methanone 3k, effect on the test culture of M. luteum at a concentration of 0.5% is close to the control drug vancomycin. Moreover, [5-(4-bromophenyl)-2-methyl-7-thioxo-2,3-dihydro-7H-[1,3]thiazolo[3,2-c]pyrimidin-8-yl](phenyl)methanone 3j has an antibacterial effect on the specified test culture at a minimum inhibitory concentration of 15.6 ��g/mL. In turn, 1-(2-methyl-5-(thiophen-2-yl)-7-thioxo-2,3-dihydro-7H-[1,3]thiazolo[3,2-c]pyrimidin-8-yl]ethanone 3d can be considered promising for further structural modification to enhance the antioxidant effect. The structure of all synthesized substances was established by spectral analysis (1H and 13C NMR, LC���MS, and FT-IR). Additionally, the structure of compound 3i was confirmed by X-ray diffraction analysis. |
