Synthesis, transformation and preliminary bioassay of 3-(thiazol-2-yl(p-tolyl)amino)propanoic acid derivatives

  • Birutė Sapijanskaitė-Banevič
  • Birutė Grybaitė
  • Rita Vaickelionienė
  • Ingrida Bružaitė
Keywords: thiazole, β-amino acids, chalcone, antibacterial activity


1,3-Thiazole is one of the most attractive cores in heterocycles chemistry and drug discovery. Its widespread use in diverse medicinal substances makes thiazole a versatile scaffold, which leads to the novel generation of efficient pharmaceuticals. This study was intended to synthesize a series of N,N-disubstituted aminothiazole derivatives having various fragments at the 4th and 5th positions of the thiazole ring. The formation of such derivatives was carried out via the Hantsch reaction, condensation reactions with various aldehydes, bromination and formation of the chalcone-type derivatives. Another goal of this study was to investigate the antibacterial properties of the obtained compounds against some gram-positive Bacillus species such as B. coagulans, B. subtilis and B. megaterium and gram-negative Escherichia coli. As it is shown by our studies in recent years, the synthesized thiazoles can serve for future development of potent thiazole derivatives for various medicinal targets.

Organic Chemistry