Abstract
Ethyl-4,5,6,7-tetrahydro-2-isothiocyanato-1-benzothiophene-3-carboxylate 1 reacts with α-amino acids to give thienopyrimidinone derivatives 12-21 with the nitrogen of the amino acid component being incorporated into the fused pyrimidine ring at position three. The synthesized compounds were characterised by elemental analysis, IR, and in typical instances also by
1
H-NMR and mass spectra. The compounds were screened for their antimicrobial activity and most of them showed a remarkably good activity against the tested microorganisms. The preliminary biochemical screening of the prepared compounds 12-21 revealed no appreciable changes of serum triglycerides and phospholipids at doses (0.004, 0.04, 0.4 mg/100 g body weight). Only the glycine 12, serine 18, methionine 19 and glutamic 20 derivatives showed significant changes in serum triglycerides, while at doses 1.0 and 2.0 mg/100 g body weight most of the compounds caused variable and significant changes in both triglycerides and phospholipids. The methionine 19 and glutamic 20 derivatives showed the most radioprotective effect on serum albumin.