The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids
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...
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National Academy of Sciences of Ukraine and Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine.
2015-10-01
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doaj-84241712f8a741b9b4fca1c1943009082020-11-24T22:30:06ZengNational Academy of Sciences of Ukraine and Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine.Ukrainian Biochemical Journal2409-49432413-50032015-10-01875829210.15407/ubj87.05.083The search of compounds with antiaggregation activity among S-esters of thiosulfonic acidsT. I. Halenova0 I. V. Nikolaeva1A. V. Nakonechna2K. B. Bolibrukh3 N. Y. Monka4 V. I. Lubenets5O. M. Savchuk6 V. P. Novikov7 L. I. Ostapchenko8Educational and Scientific Centre “Institute of Biology”,Taras Shevchenko National University of Kyiv, Ukraine;Educational and Scientific Centre “Institute of Biology”,Taras Shevchenko National University of Kyiv, Ukraine;Lviv Polytechnic National University, Ukraine;Lviv Polytechnic National University, Ukraine;Lviv Polytechnic National University, Ukraine;Lviv Polytechnic National University, Ukraine;Educational and Scientific Centre “Institute of Biology”,Taras Shevchenko National University of Kyiv, Ukraine;Lviv Polytechnic National University, Ukraine;Educational and Scientific Centre “Institute of Biology”,Taras Shevchenko National University of Kyiv, Ukraine;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).http://ukrbiochemjournal.org/wp-content/uploads/2015/10/Halenova_5_15.pdfADP-receptor antagonistsaggregationantithrombotic agentsplateletsthiosulfonic acid derivatives |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
T. I. Halenova I. V. Nikolaeva A. V. Nakonechna K. B. Bolibrukh N. Y. Monka V. I. Lubenets O. M. Savchuk V. P. Novikov L. I. Ostapchenko |
spellingShingle |
T. I. Halenova I. V. Nikolaeva A. V. Nakonechna K. B. Bolibrukh N. Y. Monka V. I. Lubenets O. M. Savchuk V. P. Novikov L. I. Ostapchenko The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids Ukrainian Biochemical Journal ADP-receptor antagonists aggregation antithrombotic agents platelets thiosulfonic acid derivatives |
author_facet |
T. I. Halenova I. V. Nikolaeva A. V. Nakonechna K. B. Bolibrukh N. Y. Monka V. I. Lubenets O. M. Savchuk V. P. Novikov L. I. Ostapchenko |
author_sort |
T. I. Halenova |
title |
The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids |
title_short |
The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids |
title_full |
The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids |
title_fullStr |
The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids |
title_full_unstemmed |
The search of compounds with antiaggregation activity among S-esters of thiosulfonic acids |
title_sort |
search of compounds with antiaggregation activity among s-esters of thiosulfonic acids |
publisher |
National Academy of Sciences of Ukraine and Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine. |
series |
Ukrainian Biochemical Journal |
issn |
2409-4943 2413-5003 |
publishDate |
2015-10-01 |
description |
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). |
topic |
ADP-receptor antagonists aggregation antithrombotic agents platelets thiosulfonic acid derivatives |
url |
http://ukrbiochemjournal.org/wp-content/uploads/2015/10/Halenova_5_15.pdf |
work_keys_str_mv |
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