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Novel Substituted Azoloazines with Anticoagulant Activity.
Alexander A Spasov1, Olga V Fedorova2, Nikolay A Rasputin2
1Department of Pharmacology & Bioinformatics, Scientific Center for Innovative Drugs, Volgograd State Medical University, Volgograd 400131, Russia.
International Journal of Molecular Sciences
|November 14, 2023
Summary
New anticoagulants are needed for infections like COVID-19. Novel 1,2,4-triazolo[1,5-a]pyrimidines show potent anticoagulant effects, with one compound exceeding dabigatran
Area of Science:
- Medicinal Chemistry
- Organic Chemistry
- Pharmacology
Background:
- Hypercytokinemia (cytokine storm) in infections like COVID-19 increases thrombosis risk.
- Current anticoagulants have safety limitations for COVID-19 patients.
- New anticoagulants with combined activities are needed.
Purpose of the Study:
- To synthesize novel substituted azoloazines.
- To evaluate their anticoagulant and other potential activities.
- To identify compounds effective against thrombosis in inflammatory conditions.
Main Methods:
- Synthesis of novel substituted azoloazines.
- In vitro evaluation of anticoagulant activity.
- Comparison with reference anticoagulant dabigatran etexilate.
- Assessment of thrombin inhibition (factor IIa).
Main Results:
- Two 1,2,4-triazolo[1,5-a]pyrimidine derivatives showed significant anticoagulant activity.
- One compound, 7,5-Di(2-thienyl)-4,5-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine, surpassed dabigatran by 2.2 times in prolonging thrombin time.
- This compound inhibits thrombin (factor IIa) and its effect is enhanced during systemic inflammation.
Conclusions:
- Novel 1,2,4-triazolo[1,5-a]pyrimidines possess potent anticoagulant properties.
- 7,5-Di(2-thienyl)-4,5-dihydro-[1,2,4]triazolo[1,5-a]pyrimidine is a promising candidate for anticoagulant therapy.
- These compounds may offer therapeutic benefits for thrombosis associated with infections and inflammatory conditions.
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