Antiviral Potential of Extracts (Prepared by Repercolation) Against Influenza A (H1N1) Virus.

An antiviral effect of extracts prepared from aerial parts of nine species and from leaves of two species of the genus L. was investigated for potential antiviral activity toward influenza A (H1N1) virus. The toxicity of dry extracts was analyzed, and the most selective extract was identified in vitro.

Synthesis of isomeric 4-(-methyltetrazolylamino)-2-phenyl-4-thiopyrano[2,3-]quinoline-3-carbaldehydes and 4-hydroxy-2-phenyl-4-thiopyrano[2,3-]quinoline-3-carbaldehyde based on tandem thiol-Michael and (aza)-Morita-Baylis-Hillman reactions and an study of the activity of the obtained compounds against influenza virus.

Unlabelled: 3-{[(1-Methyl-1-tetrazol-5-yl)imino]methyl}quinoline-2-thiol and 3-{[(2-methyl-2-tetrazol-5-yl)imino]methyl}quinoline-2-thiol were synthesized. The sequence of the thiol-Michael reaction and the (aza)-Morita-Baylis-Hillman reaction yielded 4-[(1-methyl-1-tetrazol-5-yl)amino]-2-phenyl-4-thiopyrano[2,3-]quinoline-3-carbaldehyde, 4-[(2-methyl-2-tetrazol-5-yl)amino]-2-phenyl-4-thiopyrano[2,3-]-quinoline-3-carbaldehyde, and 4-hydroxy-2-phenyl-4-thiopyrano[2,3-]quinoline-3-carbaldehyde. Cytotoxicity and antiviral activity against the A/Puerto Rico/8/34 (H1N1) influenza virus strain in MDCK cell culture were determined for the obtained compounds.

Synthesis, structure, and antiviral properties of novel 2-adamantyl-5-aryl-2-tetrazoles.

Unlabelled: The reaction of 5-aryl--tetrazoles with adamantan-1-ol in concentrated sulfuric acid proceeds regioselectively with the formation of the corresponding 2-adamantyl-5-aryl-2-tetrazoles. Nitration of these compounds leads to 2-(adamantan-1-yl)-5-(3-nitroaryl)-2tetrazoles. The structures and composition of the obtained novel 2-adamantyl-5-aryltetrazoles were proven by IR spectroscopy, H and C NMR spectroscopy, high-resolution mass spectrometry, and also by X-ray structural analysis.

Synthesis and antiviral activity of nonannulated tetrazolylpyrimidines.

Nonannulated tetrazolylpyrimidines in the structure of which the heterocyclic fragments are separated by hydrazinocarbonylmethyl, methylpyrazolyl groups or a sulfur atom were synthesized. Some of these compounds showed moderate activity against H1N1 subtype of influenza A virus. The selectivity index of the anti-influenza action of {5-[(4,6-dimethylpyrimidin-2-yl)sulfanyl]-1-tetrazol-1-yl}acetic acid, which has very low cytotoxicity, was twice as high as the selectivity index of the reference drug rimantadine.

Methods of Synthesis and Antiviral Activity of New 4-Alkyl-3-Nitro-1,4-Dihydroazolo[5,1-][1,2,4]Triazin-4-ols.

Unlabelled: An azo coupling reaction of α-nitro ketones with 5-diazoazoles was used to obtain 4-alkyl-3-nitro-1,4-dihydroazolo[5,1-][1,2,4]triazines, which were characterized with respect to their antiviral activity against influenza and Coxsackie B3 viruses.

Supplementary Information: The online version contains supplementary material available at 10.1007/s10593-021-02926-2.

7-Imidazolyl-substituted 4'-methoxy and 3',4'-dimethoxy-containing polyfluoroflavones as promising antiviral agents.

A simple and convenient method for the synthesis of new methyl 2-(4-methoxyphenyl)- and 2-(3,4-dimethoxyphenyl)-4-oxo-4-polyfluorochromen-3-carboxylates as analogs of natural methoxy-containing flavones is proposed. As a result of their directed modification under basic conditions, 7-imidazolyl-substituted derivatives were obtained. In aqueous-organic medium under basic conditions, 5,6,7,8-tetrafluoro-3-(methoxycarbonyl)flavones were transformed into 6,8-difluoro-5-hydroxy-7-(1-imidazol-1-yl)-3-(methoxycarbonyl)flavones as a result of rearrangement, while 6,7,8-trifluorinated analogs underwent a rearrangement to give 6,8-difluoro-3-(hydroxyarylidene)-7-(1-imidazol-1-yl)coumarins under the same conditions.

5-Chloro-2-thiophenyl-1,2,3-triazolylmethyldihydroquinolines as dual inhibitors of Mycobacterium tuberculosis and influenza virus: Synthesis and evaluation.

This study describes synthesis and evaluation of novel 5-Chloro-2-thiophenyl-1,2,3-triazolylmethyldihydroquinolines 7a-o as dual inhibitors of Mycobacterium tuberculosis and influenza virus. Huisgen's [3+2] dipolar cycloaddition of 6-(azidomethyl)-5-chloro-2-(thiophen-2-yl)-7,8-dihydroquinoline 5 with various alkynes 6a-o using sodium ascorbate and copper sulphate gave new dihydroquinoline-1,2,3-triazoles 7a-o in good to excellent yields. The new compounds were evaluated for in vitro antimycobacterial against M.

Single-stage synthesis of heterocyclic alkaloid-like compounds from (+)-camphoric acid and their antiviral activity.

An effective technique for one-stage synthesis of new polycyclic nitrogen-containing compounds has been developed. The procedure involves refluxing mixtures of camphoric acid with aliphatic or aromatic diamine without catalysts. In cases where the starting amine has a low boiling point (less than 200 °C), phenol is used as a solvent, as it is the most optimal one for obtaining products with good yields.