A5101588691- Quinazolinone synthesis and applications
- Synthesis and biological activity
- Eicosanoids and Hypertension Pharmacology
- Adipose Tissue and Metabolism
- Natural Antidiabetic Agents Studies
- Advanced Glycation End Products research
- Chemical Thermodynamics and Molecular Structure
- Adenosine and Purinergic Signaling
- Tryptophan and brain disorders
- Vanadium and Halogenation Chemistry
- Synthesis and bioactivity of alkaloids
- Diabetes and associated disorders
- Biochemical effects in animals
- Nitric Oxide and Endothelin Effects
- Neonatal Respiratory Health Research
- Erythropoietin and Anemia Treatment
- Cytokine Signaling Pathways and Interactions
- Berberine and alkaloids research
- Renin-Angiotensin System Studies
- S100 Proteins and Annexins
- Synthesis of heterocyclic compounds
- Ion Transport and Channel Regulation
- Wnt/β-catenin signaling in development and cancer
- Sphingolipid Metabolism and Signaling
- Lymphatic System and Diseases
Volgograd State Medical University
2017-2025
Ministry of Health of the Russian Federation
2017-2021
Samara Regional Clinical Hospital named after V.D. Seredavina
2016
Abstract Chronic inflammation is a key pathogenic driver in cardiovascular, neurodegenerative and metabolic diseases. Previously we identified highly active GSK3β inhibitors with antidiabetic potential among 3,5‐disubstituted indolin‐2‐one derivatives. We found that these derivatives also possess direct antioxidant activity, which was shown luminol‐H 2 O ABTS vitro systems IC 50 level up to 6.0 34.6 µM respectively. an essential part LPS‐induced NF‐κB NLRP3 pathways activation. Hence, the...
Nitric oxide as a therapeutic approach to the treatment of cardiovascular diseases attracted attention researchers at end 19th century. As vasodilator, nitric may be unique agent for hypertension and, result, renal failure and left ventricular hypertrophy. The aim article is analyze literature data on possible ways modulating activity various synthases an endothelial dysfunction. Materials methods. When searching materials writing review article, such abstract databases PubMed, Google...
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 Na+/H+ exchanger isoform 1 (NHE-1) attracts ongoing attention as a validated drug target for the management of cardiovascular and ocular diseases owing to cytoprotective, anti-ischemic anti-inflammatory properties NHE-1 inhibitors. Herein we report novel inhibitors realized via functionalization N1-alkyl quinazoline-2,4(1H,3H)-dione quinazoline-4(3H)-one with N-acylguanidine or 3-acyl(5-amino-1,2,4-triazole) side chain. Lead compounds show activity in nanomolar range. Their...
The aim of this study was to investigate genetic features patients with cystic fibrosis (CF) according the National Register findings in Russia. Methods. involved 2,131 CF living 74 regions Russia who were included 2014. Results . Genetic testing performed 89% patients. total mutant allele frequency 81.2%. One hundred and twenty two mutations found which comprised 173 genotypes; «mild» took 23%. most common frequencies descending order as follows: F508del, 51.53%; СFTRdele2,3, 5.93%; E92K,...
We studied the effects of a new glutamic acid derivative, glufimet, on oxidative stress, activity antioxidant enzymes, mitochondrial respiration, endothelial vasodilation and anti-platelet in female rats after exposure to 24-hour immobilization pain stress 7-nitroindazole, neuronal nitric oxide synthase (nNOS) inhibitor. A single dose administration glufimet (29 mg/kg intraperitoneally) 10 minutes before caused decrease NO metabolites serum (by 27.2%) heart homogenate (33.5% (p£0.05),...
Abstract After preliminary ab initio calculations, 3‐phenacyl substituted thiazolium salts, analogs of Alagebrium, were synthesized and investigated in vitro as glycation reaction inhibitors. The most part investigations focused on the potential title compounds to attenuate formation fluorescent AGEs well their ability disrupt cross‐linking among glycated proteins. Additionally, capability salts deglycate early products with nitroblue tetrazolium was determined. Cytotoxicological properties...
We studied the effects of a new glutamic acid derivative, glufimet, on oxidative stress, activity antioxidant enzymes, mitochondrial respiration, endothelial vasodilation and anti-platelet in female rats after exposure to 24-hour immobilization pain stress 7-nitroindazole, neuronal nitric oxide synthase (nNOS) inhibitor. A single dose administration glufimet (29 mg/kg intraperitoneally) 10 minutes before caused decrease NO metabolites serum (by 27.2%) heart homogenate (33.5% (p£0.05),...
Quinazolines are a rich source of bioactive compounds. Previously, we showed NHE-1 inhibitory, anti-inflammatory, antiplatelet, intraocular pressure lowering, and antiglycating activity for series quinazoline-2,4(1H,3H)-diones quinazoline-4(3H)-one guanidine derivatives. In the present work, novel N1,N3-bis-substituted quinazoline-2,4(1H,3H)-dione derivatives bearing two moieties were synthesized pharmacologically profiled. The most potent inhibitor 3a also possesses antiplatelet...
Aim.Glaucoma is a whole group of diseases caused by increased intraocular pressure (IOP), leading to atrophy the optic nerve and irreversible blindness. Melatonin has wide range biological activity, including antioxidant antiglaucoma, but its use limited insufficient stability duration action. To search for new, more effective antiglaucoma agents among derivatives 3-arylidene-2-oxindole, melatonin analogues, quinonoxidoreductase 2 (NQO2) inhibitors was performed, activity determined effect...
According to statistics, from 5 17 % of endoprothesis is performed for avascular necrosis. This article demonstrates the use autologous bone marrow aspirate concentrate as an orthobiological material in treatment developed stage 2 necrosis while taking glucocorticosteroids Covid-19 applying example a clinical case. The patient’s complaints, results laboratory and instrumental investigations, technique performing intraosseous injection are described. functional state knee joint was assessed...
ABSTRACT Preliminary ab initio calculations led to the synthesis of novel substituted thiazolium salts, analogs Alagebrium, which were further explored in vitro for their potential as inhibitors glycation reaction utilizing three distinct assays: inhibition fluorescent AGEs formation, anticrosslinking, and deglycation. Despite unidirectionality assays, differences observed mechanisms interference activity manifestation by compounds. The gathered data permitted formation hypotheses about...
An indisputable criterion for the chronicity of pyelonephritis is damage to tubulointerstitial tissue kidneys. One factors adverse course an increase in level b-2 microglobulin blood and urine patients. concentration serum b2-MG occurs with impaired renal function at glomerular level, content peptide indicates tubular lesions. Therefore, studies pathogenetic features development inflammatory kidney diseases against background concomitant diabetes mellitus order study corrective effect drugs...
From derivatives of quinazolin-4 (3H) -one, 2 substances were isolated: VMA-13-15 (N-[2-[4-oxo-3(4H)-quinazolinyl] propionyl]guanidine) and VMA-13-17 (N-[2-[6-bromo-4-oxo-3(4H)-quinazolinyl]acetyl]guanidine). With the therapeutic administration compounds, survival rate neurological condition animals with bilateral occlusion common carotid arteries better than in control group. Also 72 hours after surgery treatment, level cerebral blood flow severity reactions vessels to introduction a...