Triazavirin—A Novel Effective Antiviral Drug

Чупахин, О. Н.; Русинов, В. Л.; Вараксин, Михаил В.; Ulomskiy, E. N.; Саватеев, Константин В.; Butorin, Ilya I.; Du, Weijie; Sun, Zhuo; Charushin, Valery N.

doi:10.3390/ijms232314537

Cited by 21 publications

(6 citation statements)

References 54 publications

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“…164 Additionally, these agents may help curb the already existing spread in patients and prevent some of the complications such as the frequent postherpetic neuralgia that most often affects the elderly and immunocompromised patients. 165 One of the most promising developments on the VZV therapy horizon is the discovery of the bicyclic nucleoside analogues such as FV-100. It is a relatively new compound developed specifically for VZV therapy with a promising perspective to be much more effective than existing agents, such as acyclovir.…”

Section: Novel Antiviral Agentsmentioning

confidence: 99%

Varicella‐zoster virus‐related neurological complications: From infection to immunomodulatory therapies

Hakami,

Khan,

Abdulaziz

et al. 2024

Reviews in Medical Virology

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The Varicella‐zoster virus (VZV), classified as a neurotropic member of the Herpesviridae family, exhibits a characteristic pathogenicity, predominantly inducing varicella, commonly known as chickenpox, during the initial infectious phase, and triggering the reactivation of herpes zoster, more commonly recognized as shingles, following its emergence from a latent state. The pathogenesis of VZV‐associated neuroinflammation involves a complex interplay between viral replication within sensory ganglia and immune‐mediated responses that contribute to tissue damage and dysfunction. Upon primary infection, VZV gains access to sensory ganglia, establishing latent infection within neurons. During reactivation, the virus can spread along sensory nerves, triggering a cascade of inflammatory mediators, chemokines, and immune cell infiltration in the affected neural tissues. The role of both adaptive and innate immune reactions, including the contributions of T and B cells, macrophages, and dendritic cells, in orchestrating the immune‐mediated damage in the central nervous system is elucidated. Furthermore, the aberrant activation of the natural defence mechanism, characterised by the dysregulated production of immunomodulatory proteins and chemokines, has been implicated in the pathogenesis of VZV‐induced neurological disorders, such as encephalitis, myelitis, and vasculopathy. The intricate balance between protective and detrimental immune responses in the context of VZV infection emphasises the necessity for an exhaustive comprehension of the immunopathogenic mechanisms propelling neuroinflammatory processes. Despite the availability of vaccines and antiviral therapies, VZV‐related neurological complications remain a significant concern, particularly in immunocompromised individuals and the elderly. Elucidating these mechanisms might facilitate the emergence of innovative immunomodulatory strategies and targeted therapies aimed at mitigating VZV‐induced neuroinflammatory damage and improving clinical outcomes. This comprehensive understanding enhances our grasp of viral pathogenesis and holds promise for pioneering therapeutic strategies designed to mitigate the neurological ramifications of VZV infections.

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Section: Novel Antiviral Agentsmentioning

confidence: 99%

Varicella‐zoster virus‐related neurological complications: From infection to immunomodulatory therapies

Hakami,

Khan,

Abdulaziz

et al. 2024

Reviews in Medical Virology

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“…Dimethyl (27), 401 [M] +. (100), 370 (26), 369 (71), 338 (30), 337 (32), 283 (16), 282 (34), 281 (21), 152 (19), 151 (13), 126 (13), 77 (24) (20), 479 (59), 449 (61), 447 (60), 362 (30), 360 (28), 152 (35), 151 (45), 150 (67), 125 (25), 104 (51), 103 (36) (17), 398 (14), 397 (25), 382 (43), 366 (44), 365 (59), 310 (23), 309 (26), 165 (13), 104 (16), 103 (17), 77 (33) (30), 431 [M] +. (100), 416 (17), 400 (16), 399 (29), 368 (35), 367 (30), 312 (19), 183 (14), 170 (14), 77 (33) (32), 387 (45), 332 (15), 331 (23), 202 (11), 127 (10), 77 (33) (30), 445 [M] + (100), 430 (16), 414 (15), 413 (28), 382 (31), 381 …”

Section: Generalmentioning

confidence: 99%

“…(100), 416 (17), 400 (16), 399 (29), 368 (35), 367 (30), 312 (19), 183 (14), 170 (14), 77 (33) (32), 387 (45), 332 (15), 331 (23), 202 (11), 127 (10), 77 (33) (30), 445 [M] + (100), 430 (16), 414 (15), 413 (28), 382 (31), 381 (27), 326 (19), 325 (12), 223 (12) (21), 375 (49), 344 (26), 343 (23), 289 (13), 288 (30), 152 (16), 151 (12), 77 (12) (26), 437 [M] +. (100), 406 (13), 405 (26), 374 (35), 373 (36), 318 (21), 317 (15), 139 (10) (24), 435 [M] + (100), 405 (26), 404 (28), 403 (74), 3763 (23), 372 (38), 371 (39), 318 (25), 317 (32), 316 (51), 280 (28), 254…”

Section: Generalmentioning

confidence: 99%

“…Pyrrolo[2,1-f ][1,2,4]triazine derivatives can be regarded as structural analogues of non-nucleoside antiviral drugs, namely riamilovir (Triazavirin ® ) (Figure 1A). The latter has recently been registered as an antiviral drug and approved for medical treatment of influenza, ARVI and manifestations of tick-borne encephalitis virus fever [23]. The previously studied pyrrolotriazines demonstrate a relatively low cytotoxicity and are characterized by high selectivity indices against influenza virus A/Puerto Rico/8/34 (H1N1) (Figure 1B) [24].…”

Section: Introductionmentioning

confidence: 99%

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Bioactive Pyrrolo[2,1-f][1,2,4]triazines: Synthesis, Molecular Docking, In Vitro Cytotoxicity Assay and Antiviral Studies

Mochulskaya,

Kotovskaya,

Butorin

et al. 2023

Chemistry

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A series of 2,4-disubstituted pyrrolo[2,1-f][1,2,4]triazines containing both aryl and thienyl substituents were synthesized by exploiting the 1,3-cycloaddition reaction of N(1)-ethyl-1,2,4-triazinium tetrafluoroborates with dimethyl acetylenedicarboxylate. The antiviral activity of the synthesized compounds against influenza virus strain A/Puerto Rico/8/34 (H1N1) was studied in experiments on Madin-Darby canine kidney (MDCK) cell culture. Among the pyrrolo[2,1-f][1,2,4]triazine derivatives, compounds with low toxicity and high antiviral activity were identified. Dimethyl 4-(4-methoxyphenyl)-7-methyl-2-p-tolylpyrrolo[2,1-f][1,2,4]triazine-5,6-dicarboxylate was found to demonstrate the best antiviral activity (IC50 4 µg/mL and selectivity index 188). Based on the results of in vitro tests and molecular docking studies performed, a plausible mechanism of action for these compounds was suggested to involve inhibition of neuraminidase.

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“…К настоящему моменту механизм действия реамиловира до конца не изучен, наиболее вероятным считается ингибирование протеиндисульфид-изомеразы, отвечающей за образование и изомеризацию дисульфидных связей. Данные молекулярного моделирования показали, что повидимому существуют две возможные мишени: РНК-зависимая РНК-полимераза и 3C-подобная протеаза [6]. Вычислительные методы in silico выявили удовлетворительную аффинность связывания лиганда риамиловира со структурными (E)-и (S)-белками, неструктурной 3-химотрипсиноподобной протеазой (3-CLpro) SARS-CoV-2, а также человеческим ангиотензин-I превращающим ферментом-2 [8], позволяющим, по-видимому, инактивировать вирус.…”

Section: результаты и обсуждениеunclassified

Some results of riamilovir (triazavirine) usage in medical staff for prevention and treatment of COVID-19

Berdiugina,

Gusev

2023

Russian Journal of Immunology

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Riamilovir, a drug registered in Russia (chemical formula: methylthionitrooxodihydrotriazolotriazinide sodium, trade name: Triazavirin) is a synthetic analogue of guanine and a drug of direct antiviral action. Currently, there are conflicting data regarding usage of riamilovir as a preventive and therapeutic agent in coronavirus infections. The purpose of this study was to analyze some results of riamilovir usage, both for prevention of the SARS-CoV-2 infection and for the treatment of COVID-19 during the first wave of the new coronavirus pandemic. The analysis was based on a survey of 62 medical staff workers at a single medical institution in Ekaterinburg who was ill with COVID-19, being divided into 4 groups: (1) those who did not receive riamilovir (control), (2) persons who received riamilovir only as a disease prevention, (3) subjects who received the drug as a therapeutic agent, (4) those who received riamilovir before and during the disease. The data concerning usage of riamilovir for the prevention of infection with the SARS-CoV-2 virus have shown the following consequences: increased duration of hospitalization, an increased incidence of COVID-19 complications, i.e., fever, shortness of breath, pulmonary insufficiency, pneumonia, higher frequency of neurological disorders, which were not reported elsewhere. Severe clinical course of the disease was observed much more often in cases of prophylactic riamilovir administration, and the rehabilitation period was incomplete 2 months after the disease. Clinical symptoms of muscle and joint pain were documented at later terms in all persons who received riamilovir to prevent a new coronavirus infection. Usage of riamilovir for therapeutic purposes made it possible to avoid the development of pulmonary insufficiency, severe course of the infectious disease, and entirely restore the state of health. The study did not reveal the usefulness of riamilovir for prevention of COVID-19 complications when taking the drug before infection with the SARS-CoV-2 virus. However, the use of riamilovir for therapeutic purposes prevents development of severe clinical cases and is associated with 4-fold reduced risk of pain in muscles, joints, and spine among the COVID-19 patients.

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Triazavirin—A Novel Effective Antiviral Drug

Cited by 21 publications

References 54 publications

Varicella‐zoster virus‐related neurological complications: From infection to immunomodulatory therapies

Varicella‐zoster virus‐related neurological complications: From infection to immunomodulatory therapies

Bioactive Pyrrolo[2,1-f][1,2,4]triazines: Synthesis, Molecular Docking, In Vitro Cytotoxicity Assay and Antiviral Studies

Some results of riamilovir (triazavirine) usage in medical staff for prevention and treatment of COVID-19

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