A5101561449- Crystal Structures and Properties
- Chemical Synthesis and Characterization
- Zeolite Catalysis and Synthesis
- Synthesis and biological activity
- X-ray Diffraction in Crystallography
- Inorganic Fluorides and Related Compounds
- Radioactive element chemistry and processing
- Natural Antidiabetic Agents Studies
- Listeria monocytogenes in Food Safety
- Advanced Condensed Matter Physics
- Essential Oils and Antimicrobial Activity
- Natural product bioactivities and synthesis
- Nuclear materials and radiation effects
- Advanced Glycation End Products research
- Synthesis and Characterization of Heterocyclic Compounds
- Quinazolinone synthesis and applications
- Polyoxometalates: Synthesis and Applications
- Free Radicals and Antioxidants
- Bioactive Compounds and Antitumor Agents
- Synthesis of Tetrazole Derivatives
- Inorganic Chemistry and Materials
- Inorganic and Organometallic Chemistry
- Protein Tyrosine Phosphatases
- Synthesis of heterocyclic compounds
- Mineralogy and Gemology Studies
Volgograd State Medical University
2019-2025
University of Manitoba
1998-2023
Charles River Laboratories (Netherlands)
2023
We have synthesized new melatonin analogs 4,6,11,12 based on 3-hydroxy-2-oxindoles (11) and hydroxy-free 2-oxindoles (4,6,12) evaluated their neuroprotective antioxidant properties as well ability to reduce intraocular pressure. Reductive amination was used obtain 5-(benzylamino)-substituted (indolin-3-yl)acetonitriles 11 (indolin-3-yl)acetic acids 12 with high yields. Compounds 4a,c, 6a 11a,d,h,j-l demonstrated IOP reduction effect in range 15-27% similar the of reference compounds timolol...
ABSTRACT A series of oleanane and ursane‐type derivatives conjugated with a tetrazole cycle were obtained by 2 + 3 cycloaddition C28‐cyanoalkyl esters sodium azide in the presence NH 4 Cl. It was shown that 2,3‐indolo‐oleanolic ursolic acids moiety exhibited strong inhibitory activity against α‐glucosidase IC 50 values 1.15 1.28 μM, respectively, being more active than marketed drug acarbose (IC 649.94 μM). also established forms hydrogen bond backbone Ser308, which allowed an explanation...
The enzyme NRH:quinone oxidoreductase 2 (NQO2) plays an important role in the pathogenesis of various diseases such as neurodegenerative disorders, malaria, glaucoma, COVID-19 and cancer. NQO2 expression is known to be increased some cancer cell lines. Since 3-arylidene-2-oxindoles are widely used design new anticancer drugs, kinase inhibitors, it was interesting study whether structures have additional activity towards NQO2. Herein, we report synthesis novel inhibitors. It demonstrated that...
A series of two new and twenty earlier synthesized branched extra-amino-triterpenoids obtained by the direct coupling betulinic/betulonic acids with polymethylenpolyamines, or cyanoethylation lupane type alcohols, oximes, amines, amides following reduction were evaluated for cytotoxicity toward NCI-60 cancer cell line panel, α-glucosidase inhibitory, antimicrobial activities. Lupane carboxamides, conjugates diaminopropane, triethylenetetramine, C3-cyanoethylated polyamine methyl betulonate...
Susceptibility of 117 L. monocytogenes strains isolated during three time periods (1950-1980; 2000-2005, and 2018-2021) to 23 antibiotics was tested by the disk diffusion method. All were sensitive aminoglycosides (gentamicin, kanamycin, neomycin, streptomycin), glycopeptides (vancomycin teicoplanin), clarithromycin, levofloxacin, amoxicillin/clavulanic acid, trimethoprim/sulfamethoxazole. Resistance clindamycin observed in 35.5% strains. carbapenems, imipenem meropenem found 4% 5% strains,...
Listeriosis is one of the most significant humans and animals foodborne infectious diseases. Here, we characterized 48 Listeria monocytogenes strains isolated in territory inner Eurasia during second half 20th century. A total 23 (52.3%) were susceptible to nine antibiotics tested, 30.43%, 15.22%, 8.7% resistant penicillin G, ampicillin, enrofloxacin, respectively. We applied multilocus sequence typing (MLST) scheme determine phylogenetic positions strains. All but strain belonged II...
A series of bifunctional Ru(III) complexes with lonidamine-modified ligands (lonidamine is a selective inhibitor aerobic glycolysis in cancer cells) was described. Redox properties were characterized by cyclic voltammetry. An easy reduction suggested perspective for these agents as their whole mechanism action seems to be based on activation metal atom reduction. New compounds demonstrated more pronounced antiproliferative potency than the parental drug; individual new cytotoxic cisplatin....
Using oleanolic acid as a starting compound, series of new oleanane-type triterpenic derivatives were synthesized via O-acylation (with nicotinic, isonicotinic, and methoxycinnamic acyl chlorides), N-amidation cyclic- or polyamines), the Mannich reaction secondary cyclic amines), Claisen–Schmidt condensation aromatic aldehydes), their potencies treatments for immunometabolic disorders investigated. The compounds evaluated against α-glucosidase PTP1B enzymes LPS-stimulated murine macrophages....
The problem of lung damage originating from excessive inflammation and cytokine release during various types infections remains relevant stimulates the search for highly effective safe drugs. biological activity latter may be associated with regulation hyperactivation certain immune cells enzymes. Here, we propose design synthesis amino derivatives 4,6- 5,7-diaryl substituted pyrimidines [1,2,4]triazolo[1,5-a]pyrimidines as promising double-acting pharmacophores inhibiting IL-6 NO....
Acute lung injury remains a challenging clinical condition, necessitating the development of novel, safe and efficient treatments. The prevention macrophage M1-polarization is viable venue to tackle excessive inflammation. We performed phenotypic screening campaign identify azolopyrimidine compounds that effectively inhibit LPS-induced NO synthesis interleukin 6 (IL-6) secretion. identified lead compound 9g inhibits IL-6 secretion with IC50 3.72 µM without apparent cytotoxicity minimal...
The inhibitory potency of the series inhibitors soluble epoxide hydrolase (sEH) based on selenourea moiety and containing adamantane aromatic lipophilic groups ranges from 34.3 nM to 1.2 μM. most active compound 5d possesses aliphatic spacers between group fragments. Synthesized compounds were tested against LPS-induced activation primary murine macrophages. prominent anti-inflammatory activity, defined as a suppression nitric oxide synthesis by LPS-stimulated macrophages, was demonstrated...
The incidence of diabetes mellitus (DM), one the most common chronic metabolic disorders, has increased dramatically over past decade and resulted in higher rates morbidity mortality worldwide. enzyme, α-Glucosidase (α-GLy), is considered a therapeutic target for treatment type 2 DM. Herein, we synthesized arylidene, heterocyclic, cyanoetoxy- propargylated derivatives quinopimaric acid (levopimaric diene adduct with p-benzoquinone) 1–50 and, first, evaluated their ability to inhibit α-GLy....
Type 2 diabetes mellitus is a chronic metabolic disorder characterized by persistent hyperglycemia, inflammation, impaired insulin secretion, and/or peripheral resistance. Current α‐glucosidase inhibitors approved for clinical use exhibit limited efficacy compared to other glucose‐lowering agents. In this study, series of mono‐ and bis‐benzylidene derivatives were synthesized via aldol condensation 3‐oxo‐dammarane triterpenoids with terephthalic aldehyde. The target derivatives, based on the...
The crystal structure of malinkoite, NaBSiO 4 , a 13.8964(4) A, c 7.7001(2) P 6 3 Z = 18, D x 2.922 g cm −3 from the Khibina–Lovozero complex, Kola peninsula, Russia, has been solved by direct methods and refined to an R index 3.8% using 2094 unique observed (| F o | > 4σ ) reflections collected with single-crystal diffractometer fitted CCD detector Mo K α X-radiation. Malinkoite is framework borosilicate consisting six-membered rings regularly alternating (SiO (BO tetrahedra, Na located in...
Totally, 45 L. monocytogenes strains isolated from meat, poultry, dairy, and fish products in the Central European part of Russia 2001-2005 2019-2020 were typed using a combined MLST internalin profile (IP) scheme. Strains belonged to 14 clonal complexes (CCs) phylogenetic lineages I II. Almost half (20 45) six CCs previously recognized as epidemic clones (ECs). ECI ECV during both studied periods, ECII, ECIV, ECVI, ECVII 2001-2005, but not 2019-2020. ECI, ECV, animal origin. ECII ECVI fish....
The combination of one molecule organic and metal-based fragments that exhibit antitumor activity is a modern approach in the search for new promising drugs. In this work, biologically active ligands based on lonidamine (a selective inhibitor aerobic glycolysis used clinical practice) were introduced into structure an organometallic ruthenium scaffold. Resistant to ligand exchange reactions, compounds prepared by replacing labile with stable ones. Moreover, cationic complexes containing two...
Carbobystrite, ideally Na 8 [Al 6 Si O 24 ](CO 3 )·4H 2 O, trigonal, a 12.6678(5), c 10.3401(4) A, V 1437.0(2) A , c:a = 0.8162, space group P 31 Z 2, R 0.0271 (for 4861 observed reflections collected with four-circle X-ray diffractometer), is new cancrinite-group mineral species from Mount Koashva, Khibina alkaline massif, Kola Peninsula, Russia. It formed in pegmatitic environment. Associated minerals are: microcline, sodalite, megakalsilite, natrolite, pectolite, aegirine, natrite,...
Paravinogradovite is a new mineral species from Mount Kukisvumchorr, Khibina alkaline massif, Kola Peninsula, Russia. forms prismatic crystals elongate along [100] and up to 0.5–1.0 cm long; in some cases occur fan-shaped aggregates sporadically scattered throughout matrix of feldspar, nepheline natrolite strongly mineralized nepheline–feldspar pegmatite. Associated minerals are nepheline, K-feldspar, albite, analcime, natrolite, aegirine, biotite, chlorite, zircon, ilmenite, pyrochlore,...
In this work, we describe the design, synthesis, and structure-activity relationship of 6-(tetrazol-5-yl)-7-aminoazolo[1,5-a]pyrimidines as inhibitors Casein kinase 2 (CK2). At first, optimized reaction conditions for azide-nitrile cycloaddition in series 6-cyano-7-aminoazolopyridimines sodium azide. The regioselectivity process has been shown, cyano group pyrimidine cycle was converted to tetrazole while nitrile azole fragment did not react. desired tetrazolyl-azolopyrimidines were obtained...
The crystal structure of end-member sogdianite from the Dara-i-Pioz alkaline massif, northern Tajikistan, a 10.1240(3), c 14.3198(5) A, V 1271.1(1) A 3 , space group P 6/ mcc Z = 2, has been refined to an R index 2.0% using 576 observed (| F o | > 4σ ) reflections collected with single-crystal diffractometer Mo K α X-radiation. Electron-microprobe analysis gives composition (Zr 1.98 Hf 002 ∑2.00 (K 0.99 Na 0.01 ∑1.00 Li 2.97 Si 12.01 O 30 . typical double-ring silicates milarite...
Nous avons resolu la structure cristalline de zeravshanite, composition ideale Cs 4 Na 2 Zr 3 (Si 1 8 O 5 )(H O) , monodinique, a 26.3511(8), b 7.5464(3), c 22.9769(8) A, β 107.237(1)°, V 4363.9(4) A groupe spatial C2/c, Z = 4. D(calc.) 3.170 g.cm - par methodes directes; nous l'avons affinee jusqu'a un residu R 2.8% en utilisant 4508 reflexions uniques observees [F o > 4σF], et mesurees avec rayonnement MOKα diffractometre Bruker P4 muni d'un detecteur CCD. Une analyse microsonde...