Abstract [eng] |
Recently, great attention of scientists has been paid to the synthesis of new biologically active compounds that could be effective in treating bacterial infections. In this project, transformations of carbonyl fragment of 3-[(2,5-dimethylphenyl)(4-aril-1,3-thiazol-2-yl)amino]propanoic acid to acid hydrazides were performed and condensations of hydrazide to heterocyclic aldehydes and moncetones were carried out. Reactions between propanoic acids and 1,2-fenilendiamine were performed and products with benzimidazole fragment were obtained. After use of HBTU reagent, compounds with sulphanilamide fragment were synthesized. The structures of newly synthesized compounds were characterised by melting point and 1H, 13C NMR, IR spectras, elemental analysis data. 3-[(2,5-Dimethylphenyl)(4-aryl-1,3-thiazol-2-yl)amino]propanoic acids and their newly derivatives were analysed for their antioxidant properties performing DPPH and FRAP assays and antibacterial activity against gram-positive Bacillus subtilis and gram-negative Escherichia coli, Rhizobium radiobacter, Xanthomonas campestris bacterial cultures were determined. High antioxidant activity, DPPH method, showed N-(2-(1H-benzo[d]imidazol-2-yl)ethyl)-4-(4chlorophenyl)-N-(2,5-dimethylphenyl)thiazol-2-amine, while FRAP method, compound – 5,8dimethyl-1-(4-(naphthalen-2-yl)thiazol-2-yl)-2,3-dihydroquinolin-4(1H)-one. 3-{[4-(3,4Dichlorophenyl)thiazol-2-yl](2,5-dimethylphenyl)amino}propanoic acid had the best antibacterial activity against Bacillus subtilis bacteria and 3-{[4-(4-chlorophenyl)thiazol-2-yl](2,5dimethylphenyl)amino}-N'-cyclopentylidenepropanehydrazide effictively inhibited gram-negative bacterial cultures. |