AI Article Synopsis

  • Hypercytokinemia, or cytokine storm, complicates treatments for viral and bacterial infections like COVID-19 and increases thrombosis risk, highlighting the need for new anticoagulants.
  • Current direct anticoagulants are limited in use for COVID-19 due to safety concerns, making the discovery of dual-action drugs with antiviral or antidiabetic properties critical, especially for patients with comorbidities like hypertension or diabetes.
  • Novel compounds, particularly a specific triazolo-pyrimidine, show promising anticoagulant effects, outperforming existing medications like dabigatran etexilate and are especially effective during systemic inflammation.

Article Abstract

Hypercytokinemia, or cytokine storm, often complicates the treatment of viral and bacterial infections, including COVID-19, leading to the risk of thrombosis. However, the use of currently available direct anticoagulants for the treatment of COVID-19 patients is limited due to safety reasons. Therefore, the development of new anticoagulants remains an urgent task for organic and medicinal chemistry. At the same time, new drugs that combine anticoagulant properties with antiviral or antidiabetic activity could be helpfull in the treatment of COVID-19 patients, especially those suffering from such concomitant diseases as arterial hypertension or diabetes. We have synthesized a number of novel substituted azoloazines, some of which have previously been identified as compounds with pronounced antiviral, antibacterial, antidiabetic, antiaggregant, and anticoagulant activity. Two compounds from the family of 1,2,4-triazolo[1,5-]pyrimidines have demonstrated anticoagulant activity at a level exceeding or at least comparable with that of dabigatran etexilate as the reference compound. 7,5-Di(2-thienyl)-4,5-dihydro-[1,2,4]triazolo[1,5-]pyrimidine has shown the highest ability to prolong the thrombin time, surpassing this reference drug by 2.2 times. This compound has also exhibited anticoagulant activity associated with the inhibition of thrombin (factor IIa). Moreover, the anticoagulant effect of this substance becomes enhanced under the conditions of a systemic inflammatory reaction.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10648877PMC
http://dx.doi.org/10.3390/ijms242115581DOI Listing

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