Based on a series of 1-indol-5-ylamines substituted in the pyrrole ring, the corresponding -(indol-5-yl)trifluoroacetamides and indol-5-ylaminium trifluoroacetates were prepared. An study showed a wide range of their biological activity, including antimicrobial, antiviral, antiprotozoal, anthelmintic, and antifungal effects. The results of and screening for antimicrobial activity correlate with each other. All compounds are capable of inhibiting the growth of the tested microorganism strains. The dependence of minimum inhibitory concentrations on the nature of the substituents at the benzene and pyrrole rings of the indole system was revealed.

A kinetic study of the effect of thermoheliox (inhalation of a helium and oxygen mixture, 70 °C) on the functional hemodynamics of the human brain by functional magnetic resonance imaging was carried out. The dynamic responses of the BOLD signal were found to be biphasic. An empirical equation describing the first phase of the hemodynamic response to visual stimulus was proposed. It was shown that preliminary inhalation of thermoheliox stimulates the hemodynamic responses by slowing down the vasoconstriction.

We optimized the process of extraction and purification of betulin from birch bark and modified preparative syntheses of the simplest derivatives of betulin, namely, betulonic acid, betulonic aldehyde, and 3-aminobetulinic acid, as a platform for subsequent modifications.

The three-component cyclization of 3-polyfluoroalkyl-3-oxopropanoates and methyl ketones with ammonium acetate affords 6-organyl-4-(polyfluoroalkyl)pyridin-2(1)-ones (organyl is alkyl, aryl, or hetaryl). The synthesized pyridones were evaluated for antifungal, antibacterial, and analgesic activity.

The kinetic characteristics of the interaction of -acetylcysteine (ASH) with reactive oxygen species (ROS), peroxyl radicals and hydrogen peroxide were determined. It was found that in terms of activity ASH in these reactions is similar to glutathione GSH, the main endogenous bioantioxidant. The kinetics of heat release in the interaction of GSH and ASH with HO was studied for the first time by isothermal calorimetry. It is shown that the kinetic curves of heat release and changes in specific heat release rates practically coincide for both thiols taken in the stoichiometric ratio in the known reaction 2 TSH + HO → TSST + 2 HO. This indicates the relative autonomy of the S-H and S-S bonds in thiols and disulfides, which are not affected by other groups in the molecule. At pH<7, ASH, like GSH, interacts with HO to form thiyl radicals, which initiate thiol-ene reactions with unsaturated phenol resveratrol. Under the same conditions, ASH ensures nearly the same radical initiation rates as GSH, and thiyl radicals from ASH are close in activity to GS in chain propagation reactions.

This review is focused on the synthetic strategies to heterocyclic -nucleosides and covers the literature from 2011 to 2021. The main attention is paid to the following three approaches: the direct C-C coupling of a carbohydrate moiety with a preformed aglycon unit, the construction of a (pseudo)sugar residue on a pre-formed aglycon, and the construction of an aglycon on a pre-formed (pseudo)sugar. In each Section, the literature data are categorized in terms of the size of aglycon from simple to complex, the advantages and drawbacks of the reviewed approaches are discussed.

The PROTAC () technology is a method of targeting intracellular proteins previously considered undruggable. This technology utilizes the ubiquitin-proteasome system in cells to specifically degrade target proteins, thereby offering significant advantages over conventional small-molecule inhibitors of the enzymatic function. Preclinical and preliminary clinical trials of PROTAC-based compounds (degraders) are presented. The review considers the general principles of the design of degraders. Advances and challenges of the PROTAC technology are discussed.

The polysaccharide mannan is the main surface antigen of the cell wall of fungi, playing an important role in the pathogenesis of diseases caused by these mycopathogens. Mannan has a complex, comb-like structure and includes a variety of structural units, with their combination varying depending on the species and strain. Glucomannan, a polysaccharide from , contains terminal -d-glucose residues attached to oligomannoside side chains. This paper describes the first synthesis of a pentasaccharide structurally related to glucomannan fragment, which is an -(1→2)-linked tetramannoside terminated at the non-reducing end by an -d-glucopyranosyl residue. The pentasaccharide was obtained as a 3-aminopropyl glycoside, which made it possible to synthesize also its biotinylated derivative, suitable for various glycobiological studies. The most complicated step in the pentasaccharide synthesis was stereoselective 1,2--glycosylation to attach the -d-glucopyranosyl residue. This was accomplished using a glucosyl donor specially developed in our laboratory, the protecting groups of which provide the necessary -stereoselectivity. The target biotinylated pentasaccharide thus obtained will be used in the future as a model antigen for the detection of immunodeterminant epitopes of mannans.

Conjugates of the natural alkaloid (a,7)-colchicine with bicyclic monoterpenoids and their derivatives were synthesized for the first time. Molecular docking of the synthesized agents in the active site of the main viral protease of the SARS-CoV-2 virus was carried out. The cytotoxic properties of the agents against different cell lines and the ability to inhibit the main viral protease 3CLPro were studied.

The multistage purposeful synthesis of 5,15-bis(4'-l--tyrosinylamidophenyl)-10,20-bis(-methylpyridin-3'-yl)porphine diiodide was carried out, and the optimum synthesis conditions were determined. 5,15-Bis(4'-nitrophenyl)-10,20-bis(pyridin-3'-yl)porphine served as the starting porphyrin. The structure, individual character, and purity of the target compound were proved by electron spectroscopy, H NMR spectroscopy, mass spectrometry (MALDI TOF), and TLC. Specific features of the interaction of the synthesized porphyrin with S-protein of SARS-CoV-2 were studied using spectral and thermochemical methods, including conditions of photoirradiation. The photoirradiation of the synthesized porphyrin in a complex with the SARS-CoV-2 S-protein can result in the partial oxidation of amino acid residues of the protein and distort its primary and secondary structures. The photoirradiation of the S-protein complex with the porphyrin decreases its thermal resistance to melting by 15 °C compared to the free S-protein and causes porphyrin release.

Based on the data obtained by molecular modeling of the non-covalent interaction of non-symmetric -benzylbispidin-9-ol amides with the active site of the main protease 3CLpro of the SARS-CoV-2 virus, a series of compounds was synthesized, and their inhibitory activity against 3CLpro was studied and compared with that of the known inhibitor ML188 (IC = 1.56±0.55 µmol L). It was found that only compound containing the 1,4-dihydroindeno[1,2-]pyrazole fragment showed moderate activity (IC = 100±5.7µmol L) and was characterized by the highest calculated binding energy among the studied bispidine derivatives according to molecular docking data.

Complex formation processes of tetrasulfosubstituted cobalt(II) phthalocyanine with ORF3a accessory protein of SARS-CoV-2 coronavirus were studied. The interaction of ORF3a protein with SARS-CoV-2 virus with tetrasulfosubstituted cobalt(II) phthalocyanine affords a stable complex in which metallophthalocyanine exists in the monomeric form. The complex formation induces slight changes in the secondary structure of the protein by increasing the fraction of disordered fragments of the polypeptide chain. The photoirradiation of the complex of ORF3a protein of SARS-CoV-2 virus with tetrasulfosubstituted cobalt(II) phthalocyanine leads to the photooxidation of amino acid residues of the protein.

Light alkenes are among the main petrochemical intermediate products, the consumption of which is steadily growing. Using ethylene as an example, the possibilities of using polyfunctional heterogeneous catalysts for carrying out practically important reactions of its oligomerization, alkylation, and metathesis were considered. Particular attention was paid to catalysts for the conversion of ethylene to propylene.

Effects of irradiation with visible light on the process of self-assembly in an aqueous l-cysteine-silver solution (CSS) and hydrogels based on were investigated using a set of physico-chemical methods. It was found that the exposure to light of CSS and hydrogels based on l-cysteine and silver acetate colors them firstly into yellow and subsequently to brown, which is due to the plasmon resonance of free electrons at the surface of resulting silver nanoparticles (AgNPs). A mechanism involving participation of AgNPs was proposed for the self-assembly in CSS and hydrogel.

Radical polymerization was used to synthesize and characterize (co)polymers with sodium styrenesulfonate (NaSS), 4-methacryloylamidosalicylic acid (MASA), and -vinylpyrrolidone, which have a low cytotoxicity and a high antiviral activity against the human respiratory syncytial virus. The interaction of copolymers with Tb ions was studied. The complexes formed in dilute aqueous solutions at a concentration of MASA units ⩽ 1 · 10 mol L demonstrate a strong luminescence. The luminescence intensity is independent of copolymer composition, but increases when the NaSS units are substituted with uncharged N-vinylpyrrolidone units. The obtained Tb polymer complexes are promising luminescent sensors for the visualization of biological objects interacting with copolymers.

Glycyrrhizic acid (GA) is the active ingredient in licorice root, which exhibits a wide range of biological activities, including anti-inflammatory and antiviral activities. In particular, the virus-inhibiting effect of GA on SARS-associated coronavirus was demonstrated. In addition, GA was found to be capable of increasing bioaccessibility of other drugs when used together. All these effects can be based on the ability of GA to incorporate into cell membranes and change their physical and functional properties. One of the possible mechanisms of the antiviral action of GA against COVID-19 is also considered to be the prevention of fusion of the virus envelope with the plasma membrane of the host cell. The interaction of GA with model lipid membranes was studied by the NMR method. Different factors influencing the incorporation of the GA molecule into the lipid bilayer (phospholipid structure, pH of the medium) were examined.

A new method for preparation of 4-hydroxy-3-nitro-1,4-dihydrotriazolo[5,1-][1,2,4]-triazines using 1-nitro-2-morpholinoethylene and 3-diazo-1,2,4-triazoles is proposed. Antiviral activity against the Coxsackie B3 virus and electrochemical transformations of the prepared compounds are studied.

Molecular modeling tools were applied to design a potential covalent inhibitor of the main protease (M) of the SARS-CoV-2 virus and to investigate its interaction with the enzyme. The compound includes a benzoisothiazolone (BZT) moiety of antimalarial drugs and a 5-fluoro-6-nitropyrimidine-2,4(1.,3)-dione (FNP) moiety mimicking motifs of inhibitors of other cysteine proteases. The BZT moiety provides a fair binding of the ligand on the protein surface, whereas the warhead FNP is responsible for efficient nucleophilic aromatic substitution reaction with the catalytic cysteine residue in the M active site, leading to a stable covalent adduct. According to supercomputer calculations of the reaction energy profile using the quantum mechanics/molecular mechanics method, the energy of the covalent adduct is 21 kcal mol below the energy of the reactants, while the highest barrier along the reaction pathway is 9 kcal mol. These estimates indicate that the reaction can proceed efficiently and can block the M enzyme. The computed structures along the reaction path illustrate the nucleophilic aromatic substitution (SAr) mechanism in enzymes. The results of this study are important for the choice of potential drugs blocking the development of coronavirus infection.

A comparative evaluation of the antiviral activity of a number of new and previously synthesized terpenophenols and their - or -containing derivatives against the A/Puerto Rico/8/34 (H1N1) virus strain was carried out. 2-Isobornylphenol, 1,2-dihydroxy-6-isobornyl-4-methylbenzene, 2-isobornyl-1,4-benzoquinone, and N-butyl-4-hydroxy-3,5-diisobornylbenzamide showed the highest activity.

(2-Chloroquinolin-3-yl)-1,3,4-thiadiazole-2-carboxamides were synthesized from hydrazones obtained the reaction of 3-formyl-2-chloroquinoline with oxamic acid thiohydrazides.

Efficient conditions for the synthesis of nitrogen-containing heterocyclic derivatives of (1,3)(+)-camphoric acid were selected. A series of heterocyclic compounds based on (+)-camphoric acid bearing pharmacophoric fragments was synthesized using the developed methodology. The compounds were tested for their antiviral activity against SARS-CoV-2 and H1N1 influenza viruses, and efficient inhibitors were identified that are of significant interest for further studies. The stability of the compounds and pharmaco-kinetics of the leader compound were studied when administered intragastrically and intramuscularly to mice at a dose of 200 mg kg using the HPLC-MS/MS method.