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Статья
Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication
2021
Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4- triazolo[5,1-c]-1,2,4-triazine-7(4Í)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4- triazolo[5,1-s]-1,2,4-triazin(e)-7(4Í)-one} was discovered inÍÅK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination. Copyright © 2010, American Society for Microbiology. All Rights Reserved.
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Версии
- 1. Version of Record от 2021-04-27
Метаданные
Название журнала
- Antimicrobial Agents and Chemotherapy
Том
- 54
Выпуск
- 5
Страницы
- 2017-2022
Ключевые слова
- ( 2 methylthio 6 amino 1,2,4 triazolo[ 5,1 s] 1,2,4 triazine 7 (4i) one; ( 2 methylthio 6 nitro 1,2,4 triazolo[ 5,1 c] 1,2,4 triazine 7 (4i) one; 1,2,4 triazine derivative; antivirus agent; rimantadine; triazavirine; triazine derivative; unclassified drug; animal cell; animal experiment; antiviral activity; area under the curve; article; blood; cell culture; chicken; chorioallantois; controlled study; death; drug bioavailability; drug distribution; drug efficacy; drug half life; drug metabolism; human; human cell; Influenza virus A; Influenza virus A H5N1; Influenza virus B; liver homogenate; maximum plasma concentration; metabolite; mouse; nonhuman; pharmacological parameters; priority journal; rabbit; time to maximum plasma concentration; virus replication; virus resistance; virus strain; Animals; Antiviral Agents; Azoles; Disease Models, Animal; Dogs; Drug Design; Hepatocytes; Humans; Influenza A virus; Influenza B virus; Injections, Intravenous; Kidney; Mice; Mice, Inbred CBA; Orthomyxoviridae Infections; Rabbits; Stomach; Triazines; Virus Replication
Тип документа
- journal article
Источник
- scopus
