Anti-Inflammatory Activity of Novel (S)-Naproxen Derivatives

© 2016, Springer Science+Business Media New York.In order to optimize the study of the anti-inflammatory activity of novel drugs, in the current study, we used simple in vitro test system, which included osmotic and free radical hemolysis of human erythrocytes and human platelets aggregation, to screen for potential anti-inflammatory activity of three newly developed (S)-naproxen derivatives. We selected one of them (L3), which performed in in vitro tests nearly as well as naproxen, and studied their anti-inflammatory effects on in vivo model of inflammation, induced by carragenan. L3 was comparable to naproxen in its anti-inflammatory effects, suggesting that the studied simple inexpensive in vitro tests of erythrocyte osmotic and free radical hemolysis and human platelets aggregation could be used for pre-screening of potential anti-inflammatory agents

SYNTHESIS AND INVESTIGATION OF POLYMERS CONTAINING ANILINE AND INDOLE FRAGMENTS

This work was supported by the Ministry of Science and Higher Education of the Russian Federation as part of the state task no. 122031400278-2

Chiral crystallization of cis-2,3-dichloro-buth-2-ene-1,4-diol

The X-ray diffraction study of cis-2,3-dichlorobuth-2-ene-1,4-diol (3) obtained by the reduction of 3,4-dichloro-5-ethoxy- and 5-isopropoxi-2(5H)- furanones with lithium aluminum hydride is performed. The crystals of compound 3 are trigonal: a = b = 15.746(9) Å, c = 6.848(4) Å; V = 1470.5(15) Å3, space group P31, Z = 9 (three independent molecules). Independent molecules have identical planar conformation, and hydroxyl groups are located on different sides of the multiple bond plane. The supramolecular motif of the crystal is spirals about the threefold screw axes; the neighboring spirals are linked by OH.O hydrogen bonds. © 2013 Pleiades Publishing, Ltd

Electrochemically driven molecular rotors based on ferrocene-1,1'-diyl-bisphosphinic acids

© 2015, Pleiades Publishing, Ltd. Based on ferrocene-1,1'-diyl-bisphosphinic acids Fc[P(R)(O)OH]2 (R = H, Me, Et, Ph) in methanol, two types of electrochemically driven molecular rotors are developed. Monoanions of acids are fixed in the cis-conformation due to the presence of an intramolecular hydrogen bond, whereas dianions are fixed in the trans-conformation due to electrostatic repulsion forces. Upon the transformation of monoanions to dianions, the controlled rotation of cyclopentadienyl rings from cis to trans-conformation occurs; the reverse switching leads to the reverse rotation. In one type of rotors, the rotation is controlled by the reversible variation of the solution pH and composition in the electrochemical oxidation-re-reduction cycle of N-phe-nyl-N'-isopropyl-1,4-phenylenediamine; in the other type, the rotation is determined by the one electron oxidation-re-reduction of the ferrocene nucleus in monoanions. The latter rotor type at room temperature can operate stably only for a short time (τ< 1 s) and at longer times is irreversibly destructed during the oxidation stage

Assessment of risk factors for fatal outcome in patients with hemorrhagic stroke

The aim of the study - to analysis of risk factors for fatal outcome in patients with hemorrhagic stroke.Цель исследования - анализ факторов риска летального исхода у пациентов с геморрагическим инсультом

Клинико-эпидемиологические аспекты работы Казанского центра экстрапирамидной патологии

Pathology of extrapyramidal nervous system (EP) is one of the most complex sections of clinical neurology. Specificity of EP disorders accounts for the necessity of specialized assistance to patients with parkinsonism, tremor, dystonias, tics and other hyperkinesias. The article gives an account of a 4-year experience of Center for Extrapyramidal pathology work, as well as its problems and achievements. A total of 1 738 patients with different motor disorders (total of 4 301 consultations) were examined in the center for the whole period of its existence. Scientific research work is carried on as well. On the basis of the experience it was found out that neurologists. Сome across considerable difficulties in making diagnosis and choice of extrapyramidal diseases treatment. We are planning to expand the use of modern techniques in diagnosis and treatment (including botulotoxin injections, deep brain stimulation), identification of epidemiology of some extrapyramidal disorders in Kazan city.Патология экстрапирамидной нервной системы представляет собой один из наиболее сложных разделов клинической неврологии. Специфичность экстрапирамидных расстройств диктует необходимость создания специализированной помощи пациентам с паркинсонизмом, тремором, дистониями, тиками и другими гиперкинезами. В данной статье описан четырехлетний опыт работы Центра экстрапирамидной патологии (г. Казань), его проблемы и успехи. За время существования центра проведено 4 301 консультация 1 738 пациентам с различными двигательными расстройствами, ведется научно-просветительская работа. Опыт работы показал, что неврологи испытывают значительные сложности в диагностике и выборе методов лечения экстрапирамидных заболеваний. Планируется расширение использования современных методов диагностики и лечения (в том числе инъекций ботулотоксина, глубокой стимуляции мозга), установление эпидемиологии отдельных экстрапирамидных заболеваний в г. Казани

Antimicrobial effects of sulfonyl derivative of 2(5H)-furanone against planktonic and biofilm associated methicillin-resistant and -susceptible Staphylococcus aureus

© 2017 Sharafutdinov, Trizna, Baidamshina, Ryzhikova, Sibgatullina, Khabibrakhmanova, Latypova, Kurbangalieva,Rozhina, Klinger-Strobel, Fakhrullin, Pletz, Bo gachev, Kayumov and Makarewicz. The gram-positive opportunistic bacterium Staphylococcus aureus is one of the most common causatives of a variety of diseases including skin and skin structure infection or nosocomial catheter-associated infections. The biofilm formation that is an important virulence factor of this microorganism renders the antibiotic therapy ineffective, because biofilm-embedded bacteria exhibit strongly increased tolerance to antimicrobials. Here, we describe a novel 3-chloro-5(S)-[(1R,2S,5R)-2-isopropyl-5-methylcyclohexyloxy]-4-[4-methylphenylsulfonyl] -2(5H)-furanone (F105), possessing a sulfonyl group and l-menthol moiety. Minimal inhibitory and bactericidal concentration values (MIC and MBC) of F105 were 10 and 40 mg/L, respectively, suggesting F105 biocidal properties. F105 exhibits pronounced activity against biofilm-embedded S. aureus and increases the efficacy of aminoglycosides (amikacin, gentamicin, and kanamycin) and benzalkonium chloride with fractional inhibitory concentration index values of 0.33-0.44 and 0.29, respectively, suggesting an alternative external treatment option, e.g., for wound infections. Moreover, low concentrations (0.5-1.3 mg/L) of F105 reduced the MICs of these antimicrobials twofold. By using confocal laser scanning microscopy and CFU counting, we show explicitly that F105 also restores the antimicrobial activity of gentamicin and ampicillin against S. aureus biofilms by several orders of magnitude. Biofilm structures were not destroyed but sterilized, with embedded cells being almost completely killed at twofold MBC. While F105 is quite toxic (CC 50 /MBC ratio 0.2), our data suggest that the F105 chemotype might be a promising starting point for the development of complex topical agents for combined anti-staphylococcal biofilm-therapies restoring the efficacy of some antibiotics against difficult to treat S. aureus biofilm

Chronic low back pain syndrome

The aim of the study – to analyse the factors of chronic low back pain.Цель исследования - анализ факторов хронизации боли в нижней части спины

Pathogenic variants in SLF2 and SMC5 cause segmented chromosomes and mosaic variegated hyperploidy

Embryonic development is dictated by tight regulation of DNA replication, cell division and differentiation. Mutations in DNA repair and replication genes disrupt this equilibrium, giving rise to neurodevelopmental disease characterized by microcephaly, short stature and chromosomal breakage. Here, we identify biallelic variants in two components of the RAD18-SLF1/2-SMC5/6 genome stability pathway, SLF2 and SMC5, in 11 patients with microcephaly, short stature, cardiac abnormalities and anemia. Patient-derived cells exhibit a unique chromosomal instability phenotype consisting of segmented and dicentric chromosomes with mosaic variegated hyperploidy. To signify the importance of these segmented chromosomes, we have named this disorder Atelís (meaning - incomplete) Syndrome. Analysis of Atelís Syndrome cells reveals elevated levels of replication stress, partly due to a reduced ability to replicate through G-quadruplex DNA structures, and also loss of sister chromatid cohesion. Together, these data strengthen the functional link between SLF2 and the SMC5/6 complex, highlighting a distinct role for this pathway in maintaining genome stability