The synthesis of new analogs of natural biologically active substances is a promising direction for the development of effective antifungal agents. Thiosulfonic acid esters (thiosulfonates) are the structural analogs of biocidal compounds from garlic, onion, cabbage, cauliflower, etc. More than 1000 thiosulfonates of various structures of the general formula RSO 2 SR' were synthesized at the Lviv Polytechnic National University, where their physicochemical properties were characterized. A high antifungal activity of the obtained substances was established in relation to the representatives of fungi of different genera. The thiosulfonates are perspective as basis for the development of effective antifungal means for the modern pharmaceutical, food industry, for the protection of various materials and agricultural products. To increase their effectiveness, antimicrobial compositions based on thiosulfonates and surfactants of microbial origin (biosurfactants) in the form of stable suspensions were developed and studied. It has been established that the use of biosurfactants in the compositions allows the enhancement of the antifungal activity of thiosulfonates and reduction of their active concentration. The possible mechanisms of the joint action of thiosulfonates and biosurfactants on fungal pathogens are proposed.
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.
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