Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities |
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Authors: | Ili? Milo? Kontogiorgis Christos Hadjipavlou-Litina Dimitra Ila? Janez Kikelj Danijel |
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Institution: | a University of Ljubljana, Faculty of Pharmacy, Ašker?eva 7, 1000 Ljubljana, Slovenia b Aristotle University of Thessaloniki, School of Pharmacy, 54124 Thessaloniki, Greece |
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Abstract: | Vascular oxidative stress, endothelial injury, and thrombosis are intertwined processes that display a synergistic pathological effect in many cardiovascular diseases. Antithrombotic therapy with anticoagulant and/or antiplatelet agents, combined with interventions against vascular oxidative stress and/or inflammation, both boosting endothelial antithrombotic potential, could display a synergistic action in the treatment of thrombosis. Of the compounds 10a-h and 11a-d, shown to possess thrombin inhibitory activity, 11a-d were found to display radical scavenging activity, 10a, 10d, and 10f were demonstrated to inhibit lipid peroxidation of linoleic acid, and 10b and 10h inhibited soybean lipoxygenase. The observed combination of thrombin inhibition with lipid peroxidation and/or lipoxygenase inhibitory activity makes compounds 10 and 11 interesting candidates for further investigations towards multiple antithrombotic drugs. |
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Keywords: | Thrombin inhibitor Antithrombotic Lipid peroxidation Lipoxygenase inhibition Radical scavenging |
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