Triazavirin—A Novel Effective Antiviral Drug
Abstract
:1. Introduction
2. Approaches to Synthesis of Triazavirin and Chemical Properties of Nitroazoloazines
2.1. Synthetic Approaches
2.2. Chemical Properties of Nitroazoloazines
- ability to form stable salts on treatment with alkali metals and amines;
- N-alkylation leading to acyclic nucleosides;
- reduction of the nitro group into the corresponding amino compounds;
- oxidation of SH and S-alkyl fragments;
- destruction of the 1,2,4-triazine ring;
- nucleophilic substitution of the nitro group.
3. Pharmacological Properties of Triazavirin
3.1. Dosage Forms
3.2. Antiviral Properties of Triazavirin
3.2.1. Activity against Influenza Virus and Toxicology Profile
3.2.2. Triazavirin for Treatment of Acute Respiratory Virus Infections (ARVI) in Adults
3.2.3. Activity against Tick-Borne Encephalitis Virus
3.2.4. Activity against SARS-CoV-2
- shortens the duration of major clinical symptoms, such as fever, and reduces the frequency of complications;
- improves patients’ responses to inflammation and hypercoagulation, reduces reliance on glucocorticoids, anticoagulants, and oxygen inhalation;
- results in a higher rate of recovery of abnormal serum bilirubin, indirect bilirubin, total protein, albumin, and uric acid levels;
- reduces use of electrolyte solutions and diuretics, resulting in less damage to liver and kidney function;
3.2.5. Molecular Modeling Studies of Triazavirin against SARS-CoV-2
4. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Group | Elimination Rate Constant, ke, Copies/g × Days | Elimination Half-Life, τ1/2, Days |
---|---|---|
Control | 0.31 | 2.21 |
Therapy with Riamilovir, 20 mg/kg, intraperitoneal, daily from 3 to 7 days after infection | 0.57 | 1.22 |
Parameter | Number of Patients n = 69 | Riamilovir Group (Number of Patients n = 34) | Ribavirin + Umifenovir Group (Number of Patients n = 35) |
---|---|---|---|
Age, years (M ± SD) | 36 ± 3 | 39 ± 3 | 32 ± 3 |
Male, (%) | 55 (79.7) | 25 (73.5) | 30 (85.7) |
Body temperature, °C (M ± SD) | 38.0 ± 0.8 | 38.0 ± 0.6 | 37.9 ± 0.9 |
Leukocytes (×109/L), (M ± SD) | 7.28 ± 1.35 | 5.76 ± 0.85 | 8.81 ± 1.54 |
Lymphocytes (×109/L), (M ± SD) | 1.6 ± 0.04 | 1.3 ± 0.02 | 2.08 ± 0.01 |
Thrombocytes (×109/L), (M ± SD) | 224 ± 13.45 | 228.39 ± 15.01 | 219.61 ± 11.74 |
Aspartate transaminase (IU/L), (M ± SD) | 29.26 ± 4.27 | 28.36 ± 3.12 | 30.21 ± 5.41 |
Alanine transaminase (IU/L), (M ± SD) | 29.37 ± 3.24 | 32.19 ± 4.34 | 26.54 ± 2.14 |
Number of Patients | Discharged by the 14th Day of Hospitalization | Not Discharged by the 14th Day of Hospitalization | Negative PCR Test after 7 Days of Hospitalization | Positive PCR Test after 7 Days of Hospitalization |
---|---|---|---|---|
Riamilovir | 21 | 13 | 26 | 8 |
Ribavirin + Umifenovir | 11 | 24 | 10 | 25 |
Overall | 32 | 37 | 36 | 33 |
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Chupakhin, O.N.; Rusinov, V.L.; Varaksin, M.V.; Ulomskiy, E.N.; Savateev, K.V.; Butorin, I.I.; Du, W.; Sun, Z.; Charushin, V.N. Triazavirin—A Novel Effective Antiviral Drug. Int. J. Mol. Sci. 2022, 23, 14537. https://doi.org/10.3390/ijms232314537
Chupakhin ON, Rusinov VL, Varaksin MV, Ulomskiy EN, Savateev KV, Butorin II, Du W, Sun Z, Charushin VN. Triazavirin—A Novel Effective Antiviral Drug. International Journal of Molecular Sciences. 2022; 23(23):14537. https://doi.org/10.3390/ijms232314537
Chicago/Turabian StyleChupakhin, Oleg N., Vladimir L. Rusinov, Mikhail V. Varaksin, Evgeny N. Ulomskiy, Konstantin V. Savateev, Ilya I. Butorin, Weijie Du, Zhiyong Sun, and Valery N. Charushin. 2022. "Triazavirin—A Novel Effective Antiviral Drug" International Journal of Molecular Sciences 23, no. 23: 14537. https://doi.org/10.3390/ijms232314537