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15 results on '"Sirotenko, V. S."'

10. Azolo[1,5-a]pyrimidines and Their Condensed Analogs with Anticoagulant Activity

Author

Savateev, K. V., Fedotov, V. V., Rusinov, V. L., Kotovskaya, S. K., Spasov, A. A., Kucheryavenko, A. F., Vasiliev, P. M., Kosolapov, V. A., Sirotenko, V. S., Gaidukova, K. A., Uskov, G. M., Savateev, K. V., Fedotov, V. V., Rusinov, V. L., Kotovskaya, S. K., Spasov, A. A., Kucheryavenko, A. F., Vasiliev, P. M., Kosolapov, V. A., Sirotenko, V. S., Gaidukova, K. A., and Uskov, G. M.

Abstract

Hypercytokinemia, or cytokine storm, is one of the severe complications of viral and bacterial infections, involving the release of abnormal amounts of cytokines, resulting in a massive inflammatory response. Cytokine storm is associated with COVID-19 and sepsis high mortality rate by developing epithelial dysfunction and coagulopathy, leading to thromboembolism and multiple organ dysfunction syndrome. Anticoagulant therapy is an important tactic to prevent thrombosis in sepsis and COVID-19, but recent data show the incompatibility of modern direct oral anticoagulants and antiviral agents. It seems relevant to develop dual-action drugs with antiviral and anticoagulant properties. At the same time, it was shown that azolo[1,5-a]pyrimidines are heterocycles with a broad spectrum of antiviral activity. We have synthesized a new family of azolo[1,5-a]pyrimidines and their condensed polycyclic analogs by cyclocondensation reactions and direct CH-functionalization and studied their anticoagulant properties. Five compounds among 1,2,4-triazolo[1,5-a]pyrimidin-7-ones and 5-alkyl-1,3,4-thiadiazolo[3,2-a]purin-8-ones demonstrated higher anticoagulant activity than the reference drug, dabigatran etexilate. Antithrombin activity of most active compounds was confirmed using lipopolysaccharide (LPS)-treated blood to mimic the conditions of cytokine release syndrome. The studied compounds affected only the thrombin time value, reliably increasing it 6.5–15.2 times as compared to LPS-treated blood. © 2022 by the authors. Licensee MDPI, Basel, Switzerland.

Published
2022

11. Prototropic equilibrium in 1(11)H-2, 3, 4, 5-tetrahydro[1, 3]diazepino[1, 2-a]benzimidazole, synthesis and pharmacological properties of its N-substituted derivatives

Author

Morkovnik, A. S., Spasov, A. A., Kuz’menko, T. A., Kucheryavenko, A. F., Divaeva, L. N., Koshchienko, Yu. V., Anisimova, V. A., Kuzmina, L. G., Rogova, N. V., Kuznetsova, V. A., Chepljaeva, N. I., Solovyova, O. A., Taran, A. S., Vorobiev, E. S., Aleshin, D. A., Sirotenko, V. S., Gajdukova, K. A., and Bogoslavtseva, M. V.

Published
2015
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15. [ANTIAGGREGANT ACTIVITY OF A NEW TRICYCLIC BENZIMIDAZOLE DERIVATIVE.]

Author

Kucheryavenko AF, Anisimova VA, Gaidukova KA, Divaeva LN, Kuz'menko TA, Morkovnik AS, Sirotenko VS, and Spasov AA

Subjects
Animals, Blood Platelets pathology, Rabbits, Benzimidazoles chemical synthesis, Benzimidazoles chemistry, Benzimidazoles pharmacology, Blood Platelets metabolism, Platelet Aggregation drug effects, Platelet Aggregation Inhibitors chemical synthesis, Platelet Aggregation Inhibitors chemistry, Platelet Aggregation Inhibitors pharmacology
Abstract

The antiaggregant activity of a new benzimidazole derivative - 2,3,4,5-tetrahydro[1,3]diazepino[1,2-α]benzimidazole (DAB-15) has been investigated in vitro in comparison to reference drugs acetylsalicylic acid (ASA) and ticlid (ticlopidine) on the models of ASA, collagen, and epinephrine induced platelet aggregation in rabbits. It was established that DAB-15 exhibited dose-dependent antiaggregant activity. On the model of ASA-induced platelet aggregation, the effect of ADB-15 exceeded that of ASA and was slightly lower than that of ticlid. On the models of collagen, and epinephrine induced platelet aggregation, DAB-15 was reliably more active than the both reference drugs.

Published
2016

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