A series of esters of 4-acetyl, 4-trifluoroacetyl- and 4-(3-chloropropionyl)aminobenzenethiosulfoacids (twenty-four compounds) were synthesized and characterized by elemental analysis, H NMR and IR spectroscopy. The antibacterial activity of the novel candidates has been screened using the agar diffusion or serial dilution methods against representative Gram-positive (, ,, sp.,), Gram-negative ( sp., ,, ,, ) bacteria and fungi (, ,, ,, ,, ). Particular potency has been discovered against all tested pathogenic bacteria and fungi by compounds and at nanomolar concentrations. Some appropriate effect of thiosulfoesters structure upon their antimicrobial activity was determined.
Thiosulfonate derivatives based on quinones were synthesized for studying “structure-activity relationship” compounds with an acylated and a free amino-group. Anti-platelet activity of the synthesized compounds was determined and the influence of substituents on the activity of the derivatives was assessed.
The optimisation of reaction conditions for obtaining thiosulfonate derivatives was performed. S,N-binucleophiles (sodium salts of 4-amino-and 4-acetylaminobenzenethiosulfonic acids) were used. The parameters of the reaction for the synthesis of derivatives by a thiosulfonate fragment were determined. Thiosulfonate derivatives based on a number of quinones and quinoxalines were synthesized.
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