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  • Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities.

Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities.

Bioorganic & medicinal chemistry letters (2011-07-16)
Miloš Ilić, Christos Kontogiorgis, Dimitra Hadjipavlou-Litina, Janez Ilaš, Danijel Kikelj
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Nordihydroguaiaretic acid, ≥97.0% (HPLC)
Sigma-Aldrich
Caffeic acid, ≥98.0% (HPLC)
Supelco
Caffeic acid, matrix substance for MALDI-MS, ≥99.0% (HPLC)