The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids

Abstract

According to the current understanding, the hyperactivation of platelets may lead to increased intravascular coagulation and thrombosis. Today a relevant issue is the search for new anti-thrombotic agents that are able to modulate the activity of platelet receptors, thus, influence the processes of activation and aggregation of platelets. The aim of this study was to investigate the effects of newly synthesized thiosulfonate derivatives on platelet aggregation. The activity of the compounds was tested in vitro using platelet-rich plasma. As a result of the screening test, structural formulas of four agents with high antiaggregative activity were established. These compounds inhibited ADP-and collagen-induced platelet aggregation in a dosedependent manner. Two of these compounds were shown to be more effective inhibitors of aggregation induced by ADP (IC 50 ~ 8-10 µM), as well as collagen (IC 50 ~ 1.5-2.0 µM).

Synthesis of Thiosulphoesters With Nitrogen Containing Fragments

“…The average forecast accuracy of the PASS program is about 85%, which is sufficient to use the data obtained to predict the spectrum of biological activity of new substances (the expected average prediction accuracy of one of the 500 types of activity is only about 0.2%) 8 . The results of the forecast provide information on the list of likely activities and the estimated probability of (Ra) presence and (Ri) absence of each activity.…”

“…32-39. 8 Lagunin А., Stepanchikova А., Filimonov D., Poroikov V. PASS: prediction of activity spectra for biologically active substances. Bioinformatics.…”

Ethylthiosulfanylate effect on Candida tropicalis

“…Some thiosulfoacid esters are promising antithrombotic agents [7]. Alkyl esters of some 4-acylaminobenzene-and heterocyclic thiosulfoacids exhibit antifungal effect towards different types of fungi (Candida albicans, Candida tropicalis, Candida рarарsilosis, Candida krusei, Candida іпсоnsрісuа, Candida поrvegensis, Candida kеfyr, Candida lusitaniae, Candida glabrata, Cryptococcus neoformans, trichosporon asahii, Geotrichum capitatum, blastoschizomyces capitatus) in low concentrations [8].…”

Modification of Alkyl Esters of 4-Aminobenzenethiosulfonic Acid by s-Triazine Fragment and Investigation of their Growth-Regulative Activity

“…Quite a few of them are offered as medicines, preservatives of fruit and vegetables, effective remedies for plant protection, growth regulators, biocidal additives, insecticides and radioprotector. [17][18][19][20][21]. In addition, thiosulfoacid esters are effective sulfenilating and sulfonylating reagents in organic synthesis, and also valuable objects for solving complex issues of molecular biology and biochemistry [17,22,23].…”