Antiviral Agents – Benzazine Derivatives

[Figure not available: see fulltext.] The review outlines the results of studies of the antiviral activity of quinoline, quinoxaline, and quinazoline derivatives published over the past 5 years. The supplied data indicate the enormous potential of benzazines for the design of effective antiviral drugs. © 2021, Springer Science+Business Media, LLC, part of Springer Nature.This work was supported by the Ministry of Science and Higher Education of the Russian Federation (project No. FEUZ-2020-0058 (N687.42B.223/20))

Synthetic approaches to 2-aryl/hetaryl- and 2-(hetaryl)ylidene derivatives of fluorinated 1,3-benzothiazin-4-ones

A series of 2-hetaryl- and 2-(hetaryl)ylidene substituted 5-fluoro-8-nitro-1,3-benzothiazin-4-ones was synthesized by interaction of 2,6-difluoro-3-nitrobenzoylisothiocyanate with C-nucleophiles. Cyclocondensation of polyfluorobenzoylchlorides with aryl and hetaryl thioamides represents new approach to 1,3-benzothiazin-4-ones. Some compounds proved to be promising for further development of tuberculostatic agents

The place of anatomical museum in teaching phisiology for non-medical specialities students: traditionsand innovations

Рассмотрен опыт сотрудничества кафедры иммунохимии УрФУ с анатомическим музеем УГМА. Проведение практических занятий по физиологии человека для студентов немедицинских специальностей на базе музея позволяет повысить наглядность преподавания и активизировать познавательную деятельность студентов.Experience of co-working of immunochemistry chair of UrFU and anatomical museum of USMA is described. Teaching physiology in museum for non-medical specialities students increases illustrativity of teaching and studying activity of students

Synthesis of new promising compounds based on pyrrolo[2,1-f][1,2,4]triazines for the prevention and treatment of socially significant viral infections

The purpose of the study is development of new approaches based on the application of the methodology of 1,3-dipolar cycloaddition to the synthesis of 2,4-diaryl-substituted pyrrolo[2,1- f] [1,2,4] triazines, promising for the prevention and treatment of socially significant viral infections.Цель исследования - разработка новых подходов, основанных на применении методологии 1,3- диполярного циклоприсоединения, к синтезу 2,4-диарилзамещенных пирроло[2,1- f][1,2,4]триазинов, перспективных для профилактики и лечения социально значимых вирусных инфекций

EFFECT OF PULSED ELECTRON-BEAM PROCESSING ON THE ANTIOXIDANT PROPERTIES OF TEA

The effect of ionizing radiation on the content of total polyphenols in tea has been studied in this research. The content oftotal polyphenols was determined with the help of ISO 14502-1:2005 using Folin-Ciocalteureagent

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

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. © 2023 by the authors.Ministry of Education and Science of the Russian Federation, Minobrnauka: 075-15-2020-777This research was supported by the Ministry of Science and Higher Education of the Russian Federation: Agreement on granting grants from the federal budget in the form of subsidies in accordance with paragraph 4 of Article 78.1 of the Budget Code of the Russian Federation (Moscow, October 1, 2020, No. 075-15-2020-777)

MnO2-Mediated Oxidative Cyclization of “Formal” Schiff’s Bases: Easy Access to Diverse Naphthofuro-Annulated Triazines

A different type of MnO2-induced oxidative cyclization of dihydrotriazines has been developed. These dihydrotriazines are considered as a “formal” Schiff’s base. This method provided easy access to naphthofuro-fused triazine via the C-C/C-O oxidative coupling reaction. The reaction sequence comprised the nucleophilic addition of 2-naphthol or phenol to 1,2,4-triazine, followed by oxidative cyclization. The scope and limitations of this novel coupling reaction have been investigated. Further application of the synthesized compound has been demonstrated by synthesizing carbazole-substituted benzofuro-fused triazines. The scalability of the reaction was demonstrated at a 40 mmol load. The mechanistic study strongly suggests that this reaction proceeds through the formation of an O-coordinated manganese complex

Dimethyl 7-Methyl-2-(Pyrrolidine-1-Yl)-4-Phenylpyrrolo[2,1-Ƒ][1,2,4]Triazine-5,6-Dicarboxylate And Dimethyl 7-Methyl-2-(4-R1-Phenyl)-4-(4-R2-Phenyl)Pyrrolo[2,1-Ƒ][1,2,4]Triazine-5,6-Dicarboxylates Exhibiting Antiviral Activity

Изобретение относится к области биологически активных соединений, обладающих противовирусным действием в отношении штамма вируса гриппа A/Puerto Rico/8/34 (H1N1) и представляющих собой диметил 7-метил-2-(пирролидин-1-ил)-4-фенилпирроло[2,1-ƒ][1,2,4]триазин-5,6-дикарбоксилат формулы (7) и диметил 7-метил-2-(4-R1-фенил)-4-(4-R2-фенил) пирроло[2,1-ƒ][1,2,4]триазин-5,6-дикарбоксилаты формулы (8) , где R1 - Me и R2 - Me; или R1 - Cl и R2 - Me; или R1 - Н и R2 - Cl. Техническим результатом является создание новых химических соединений азолоазиниевого ряда - диметил 7-метил-2-(пирролидин-1-ил)-4-фенилпирроло[2,1-ƒ][1,2,4]триазин-5,6-дикарбоксилата формулы (7) и диметил 7-метил-2-(4-R1-фенил)-4-(4-R2-фенил)пирроло[2,1-ƒ][1,2,4]триазин-5,6-дикарбоксилатов формулы (8), обладающих выраженным противовирусным действием в отношении штамма вируса гриппа A/Puerto Rico/8/34 (H1N1). 2 н.п. ф-лы, 6 пр., 2 ил.FIELD: pharmaceuticals. SUBSTANCE: invention relates to the field of biologically active compounds exhibiting antiviral effect against the strain of influenza virus A/Puerto Rico/8/34 (H1N1) and constituting dimethyl 7-methyl-2-(pyrrolidine-1-yl)-4-phenylpyrrolo[2,1-ƒ][1,2,4]triazine-5,6-dicarboxylate by the formula (7) and dimethyl 7-methyl-2-(4-R1-phenyl)-4-(4-R2-phenyl)pyrrolo[2,1-ƒ][1,2,4]triazine-5,6-dicarboxylates by the formula (8) , wherein R1 is Me and R2 is Me; or R1 is Cl and R2 is Me; or R1 is H and R2 is Cl. EFFECT: creation of new chemical compounds of the azoloazine series — dimethyl 7-methyl-2-(pyrrolidine-1-yl)-4-phenylpyrrolo[2,1-ƒ][1,2,4]triazine-5,6-dicarboxylate by the formula (7) and dimethyl 7-methyl-2-(4-R1-phenyl)-4-(4-R2-phenyl)pyrrolo[2,1-ƒ][1,2,4]triazine-5,6-dicarboxylates by the formula (8), exhibiting a significant antiviral effect against the strain of influenza virus A/Puerto Rico/8/34 (H1N1). 2 cl, 6 ex, 2 dwg

Dimethyl 7-Methyl-2-N-Tolyl-4-Phenylpyrrolo[2,1-F] [2,1,4]Triazine-5,6-Dicarboxylate with Anticoagulant Effect

Изобретение относится к новому диметил 7-метил-2-(n-толил)-4-фенилпирроло[2,1-ƒ][1,2,4]триазин-5,6-дикарбоксилату . Технический результат: получено новое соединение, обладающее антикоагулянтным действием, которое может быть использовано для предотвращения тромботических состояний при тяжелых формах вирусной инфекции. 5 ил., 3 пр.FIELD: chemistry. SUBSTANCE: invention relates to a new dimethyl 7-methyl-2-(n-tolyl)-4-phenylpyrrolo[2,1-ƒ][1,2,4]triazine-5,6-dicarboxylate . EFFECT: new compound with anticoagulant activity was obtained, which can be used to prevent thrombotic conditions in severe forms of viral infection. 1 cl, 5 dwg, 3 ex

Sulfur-containing heterocyclic compounds with potential antidi-abetic activity

Существенным звеном патогенеза СД и его осложнений является неферментативное гликозилирование белков (НГБ). Однако современная эндокринология испытывает нехватку клинически эффективных лекарственных средств для его коррекции. Проведен скрининг 23 производных 1,3,4-тиадиазина на способность ингибировать реакцию НГБ in vitro, отобраны 11 наиболее активных соединений, исследована взаимосвязь «структура - активность»