THE SEARCH OF COMPOUNDS WITH ANTIAGGREGATION ACTIVITY AMONG S-ESTERS OF THIOSULFONIC ACIDS

• Published in: Ukrainian biochemical journal 2015-09, Vol.87 (5), p.83-92
• Main Authors: Halenova, T I, Nikolaeva, I V, Nakonechna, A V, Bolibrukh, K B, Monka, N Y, Lubenets, V I, Savchuk, O M, Novikov, V P, Ostapchenko, L I
• Format: Article
• Language: English
• Subjects: ADP-receptor antagonists; aggregation; Animals; antithrombotic agents; Blood Platelets - drug effects; Cells, Cultured; Dose-Response Relationship, Drug; Drug Discovery; Esters; Molecular Structure; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - chemical synthesis; Platelet Aggregation Inhibitors - chemistry; Platelet Aggregation Inhibitors - pharmacology; Platelet-Rich Plasma - cytology; platelets; Rabbits; Structure-Activity Relationship; thiosulfonic acid derivatives; Thiosulfonic Acids - chemical synthesis; Thiosulfonic Acids - chemistry; Thiosulfonic Acids - pharmacology
• ISSN: 2409-4943; 2413-5003
• DOI: 10.15407/ubj87.05.083

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 dose-dependent manner. Two of these compounds were shown to be more effective inhibitors of aggregation induced by ADP (IC50 - 8-10 μM), as well as collagen (IC50 - 1.5-2.0 μM).