A5041279076- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Biochemical and Molecular Research
- HIV/AIDS drug development and treatment
- Asymmetric Synthesis and Catalysis
- Synthesis and Characterization of Heterocyclic Compounds
- Click Chemistry and Applications
- Garlic and Onion Studies
- Amino Acid Enzymes and Metabolism
- Cyclopropane Reaction Mechanisms
- Adenosine and Purinergic Signaling
- Catalytic C–H Functionalization Methods
- Biopolymer Synthesis and Applications
- Steroid Chemistry and Biochemistry
- Tuberculosis Research and Epidemiology
- Synthesis and Biological Evaluation
- Microbial Natural Products and Biosynthesis
- Pneumocystis jirovecii pneumonia detection and treatment
- Marine Sponges and Natural Products
- Cancer Research and Treatments
- Peptidase Inhibition and Analysis
- Oxidative Organic Chemistry Reactions
- Fungal Plant Pathogen Control
- Folate and B Vitamins Research
- Pharmacogenetics and Drug Metabolism
Engelhardt Institute of Molecular Biology
2016-2025
Russian Academy of Sciences
2015-2019
An efficient preparative method for the synthesis of siloxanols based on aerobic Co(OAc)<sub>2</sub> or Cu(OAc)<sub>2</sub>/NHPI-catalyzed oxidation hydride siloxanes has been proposed.
In recent years, a number of synthetic potentiators antibiotics have been discovered. Their action can significantly enhance the antibacterial effect and limit spread antibiotic resistance through inhibition bacterial cystathionine-γ-lyase. To expand known set potentiators, we developed methods for synthesis five new representatives 6-bromoindole derivatives—potential inhibitors cystathionine-γ-lyase—namely potassium 3-amino-5-((6-bromoindolyl)methyl)thiophene-2-carboxylate (MNS2) its...
Diallyl thiosulfinate (allicin) effectively inhibits the growth of various microorganisms, including antibiotic-resistant strains, so it can be considered to a broad-spectrum antimicrobial compound. However, its instability in bloodstream hinders use as therapeutic agent. We have synthesized number allicin analogues, both natural and synthetic, evaluated vitro their properties against Staphylococcus aureus Candida albicans. The compounds were shown exhibited more pronounced antifungal...
Acute and subchronic toxicity of the pharmacological pair based on encapsulated Citrobacter freundii C115H methionine γ-lyase enzyme/prodrug (methiin) was studied in female ICR mice. The drug showed a weak/moderate dose-dependent hepatotoxic effect. Most changes liver morphology identified were insignificant or mild deviations from norm. Long-term use single therapeutic dose per mouse 1.5 U C. @ (PEG-P(Asp)70/PLL70)-PIC-some/2 mg methiin led to slight decrease weight animals without obvious...
Cystathionine-γ-lyase (CSE) is a key enzyme for H2S generation in the pathogenic bacteria Staphylococcus aureus, Pseudomonas aeruginosa, etc. Suppression of CSE activity significantly increases antibiotic susceptibility bacteria. In this work method to synthesize novel indole-based inhibitor, 3-ammo-5-[(6-bromo-1H-indol-1-yl)methyl]thiophene, named MNS1, has been developed. The synthesis MNS1 based on modification substituted thiophene as main structural fragment, which involved alkylation...
Single-atom editing of complex molecules is steadily filling the chemical toolbox with site-selective modification reactions. Herein, a stepwise scheme for carbon-to-oxygen swap in tetralins leading to privileged chroman scaffolds presented. Increasing oxi-dation state at each stage, substrate scope naturally extends: starting from via 1-tetralones and further subsequently formed seven-membered lactones, transformation results diverse chroman-2-carboxylic acids chroman-2-ols. The effi-ciency...
Synthesis of organosilicon products with a "polar" functional group within organic substituents is one the most fundamentally and practically important challenges in today's chemistry silicones. In our study, we suggest solution to this problem, viz., high-efficiency preparative method based on aerobic Co-/N-hydroxysuccinimide (NHSI) catalyzed oxidation p-tolylsiloxanes p-carboxyphenylsiloxanes. This approach "green", commercially available, simple, inexpensive reagents employs mild reaction...
A series of novel 5′-norcarbocyclic derivatives 5-alkoxymethyl or 5-alkyltriazolyl-methyl uracil were synthesized and the activity compounds evaluated against both Gram-positive Gram-negative bacteria. The growth Mycobacterium smegmatis was completely inhibited by most active at a MIC99 67 μg/mL (mc2155) 6.7–67 (VKPM Ac 1339). Several also showed ability to inhibit attenuated strains tuberculosis ATCC 25177 (MIC99 28–61 μg/mL) bovis 35737 50–60 μg/mL), as well two virulent M. tuberculosis;...
Spiro[imidazol-5-one-4,1'-cyclopropanes] behave as donor-acceptor (D-A) cyclopropanes in a formal cycloaddition reaction with aldehydes. The activation of such type is achieved an equivalent Brønsted acid. proceeds high yields 51-92% and demonstrates moderate diastereoselectivity at the quaternary stereocenter, which determined by electron-donating nature aldehyde partner. ease separation stereoisomers allowed creation library 44 spiroannulated tetrahydrofurans various substitution patterns.
A significant increase of microbial resistance to glycopeptides (especially vancomycin-resistant enterococci and Staphylococcus aureus) prompted researchers design new semisynthetic glycopeptide derivatives, such as dual-action antibiotics that contain a molecule an antibacterial agent different class. We synthesized novel dimeric conjugates kanamycin with antibiotics, vancomycin eremomycin. Using tandem mass spectrometry fragmentation, UV, IR, NMR spectral data, it was unequivocally proven...
The reaction between simple pyridines, Michael acceptors (cyclopentenone, N-methylmaleimide), and monoalkyl-3,3-difluorocyclopropenes affords 3-(1-hydroxyindolizin-3-yl)-succinimides or 3-(1-hydroxyindolizin-3-yl)-cyclopentanones in good yields. These air-sensitive products regenerate double bond the incorporated by selective near-quantitative aerobic dehydrogenation, yielding intensively colored dyes. purple 3-(1-hydroxyindolizin-3-yl)-maleimides are highly electrophilic react smoothly with...
A new three-component reaction leading to 1-α-(pyridyl-2-[1,2,4]triazolyl)-2-alkyl-ethanones has been discovered while studying the reactivity of monosubstituted 3,3-difluorocyclopropenes in an inverse electronic demand Diels–Alder (IEDDA) cycloaddition–cycloreversion sequence with s-tetrazines. The involving above-mentioned reactants and (benzo)pyridine as a third component results complex transformation proceeding mild conditions stoichiometric ratio high functional group tolerance...
A set of 3′-modified N 4 -alkyl-5-methyl-2′-deoxycytidines has been synthesized and evaluated for biological activity. The replacement the 3′-hydroxyl group with amino, aminoethyl dialkylamino groups significantly enhances antifungal
Bacterial cystathionine γ-lyase (bCSE) is the main producer of H2S in pathogenic bacteria such as Staphylococcus aureus, Pseudomonas aeruginosa, etc. The suppression bCSE activity considerably enhances sensitivity to antibiotics. Convenient methods for efficient synthesis gram quantities two selective indole-based inhibitors, namely (2-(6-bromo-1H-indol-1-yl)acetyl)glycine (NL1), 5-((6-bromo-1H-indol-1-yl)methyl)- 2-methylfuran-3-carboxylic acid (NL2), well a synthetic method preparation...
A series of new 5'-O-carbamate prodrugs AZT have been prepared. The stability in biological media, anti-HIV properties and pharmacokinetic parameters dogs were evaluated. compounds display moderate activity cell culture. After oral administration carbamate IV dogs, both intact prodrug released discovered dog blood. Pharmacokinetic the compound estimated. Half-life (T(1/2)) after was close to that itself, time maximum concentration (T(max)) from two three times longer compared with...
α‐Ribose‐1‐phosphate (Rib‐p) and 2‐deoxy‐α‐ribose‐1‐phosphate (dRib‐p) are key intermediates in nucleoside metabolism important starting compounds for the enzymatic synthesis of various modified nucleosides. To date, chemical methods allowed preparation these rather low yields (11–37 %). This prevents their widespread use biologically active practically Here we propose to 7‐methyl‐2′‐deoxyguanosine (7‐Me‐dGuo) 7‐methylguanosine (7‐Me‐Guo) dRib‐p Rib‐p. In this paper, present effective Rib‐p...