Reaction of Picolinamides with Ketones Producing a New Type of Heterocyclic Salts with an Imidazolidin-4-One Ring

Reactions of picolinamides with 1,3-propanesultone in methanol followed by the treatment with ketones led to a series of previously unknown chemical transformations, yielding first pyridinium salts (2a–f), with a protonated endocyclic nitrogen atom, and then heterocyclic salts (3a–j) containing an imidazolidin-4-one ring. The structures of intermediate and final products were determined by IR and 1H, 13C NMR spectroscopy, and X-ray study. The effects of the ketone and alcohol structures on the product yield were studied by quantum-chemical calculations. The stability of salts 3a–j towards hydrolysis and alcoholysis makes them excellent candidates for the search for new types of biologically active compounds

Organic chemistry. History and mutual relations of universities of Russia

© 2017, Pleiades Publishing, Ltd. The review describes the history of development of organic chemistry in higher schools of Russia over a period of 170 years, since the emergence of organic chemistry in our country till now

Modern Trends of Organic Chemistry in Russian Universities

© 2018, Pleiades Publishing, Ltd. This review is devoted to the scientific achievements of the departments of organic chemistry in higher schools of Russia within the past decade

Stereochemical rearrangements of dibromides of hexacoordinated germanium containing amidomethyl and lactamomethyl chelate ligands

For the first time a slow (on the NMR time scale) dynamic exchange between two diastereomers of hexacoordinated dibromogermanes containing two amidomethyl and lactamomethyl C,O-chelate ligands has been observed at room temperature in solution. The influence of temperature and solvent on the ratio of diastereomers was studied. At higher temperatures only one set of signals of the products were detected in the NMR spectra. Based on the dynamic NMR and quantum-chemical calculations (ab initio FR 3-21G), as well as on the structures determined for these compounds in the solid state, a cis-configuration of monodentate ligands was proposed for one of the diastereomers and an all-trans-configuration for the other. At low temperatures interconversion of enantiomers in the cis-diastereomer was observed. In the case of bis[(N-methylacetamido)methyl]dibromogermane the activation and thermodynamic parameters of enantiomerization (DeltaG(298)(#) 12.0+/-0.1 kcal mol(-1), DeltaH(#) 10.7+/-0.3 kcal mol(-1), DeltaS(#) -4.6+/-2.5 cal mol(-1) K-1) and diastereomeric exchange OcCtBrcreversible arrowOtCtBrt (DeltaG(298)(#), 15.0+/-0.1 kcal mol(-1); DeltaH(#) 0.1+/-0.8 kcal mol(-1); DeltaS(#) -50.0+/-5.8 cal mol(-1) K-1; DeltaG(298)degrees -0.2+/-0.1 kcal mol(-1); DeltaHdegrees -0.8+/-0.8 kcal mol(-1); DeltaSdegrees -2.6+/-1.0 cal mol(-1) K-1) were determined. (C) 2003 Published by Elsevier Science B.V

The Effect of a New N-hetero Cycle Derivative on Behavior and Inflammation against the Background of Ischemic Stroke

Ischemic stroke triggers a whole cascade of pathological changes in the brain, one of which is postischemic inflammation. Since in such cases thrombolytic therapy is often not possible, methods that modulate inflammation and affect microglia become particularly interesting. We synthesized 3-(2-oxo-4-phenylpyrrolidin-1-yl)propane-1-sulfonate calcium(II) (Compound 4) and studied its anti-inflammatory activity in in vitro and in vivo models of inflammation and ischemia. Macrophage cell line RAW 264.7 was treated with lipopolysaccharides (LPS) and Compound 4 at various dosages to study the cytokine profile using real-time PCR and cytometric bead array (CBA). Stroke in rats was simulated by the middle cerebral artery occlusion method (MCAO). Several tests were performed to characterize the neurological deficit and locomotor activity of the rats, and afterwards, postmortem, the number of astrocytes was counted using immunohistochemistry. Compound 4 in in vitro tests dose-dependently reduced the expression of interleukin-1β (IL1β), and inducible nitric oxide synthase (iNOS) genes in cell culture and increased the concentration of cytokines: interleukin-2, 4, 6 (IL-2, IL-4, and IL-6). In vivo Compound 4 increased the orienting-exploratory behavior, and reduced neurological and motor deficit. The number of astrocytes that promote and support inflammation was lower in the group treated with Compound 4. The stroke volume measured by magnetic resonance imaging (MRI) showed no difference. We have shown that Compound 4 demonstrates anti-inflammatory activity by increasing the synthesis of anti-inflammatory and reducing pro-inflammatory cytokines, and positively affects the neurological deficit in rats. Thus, Compound 4 has a high therapeutic potential in the management of patients after a stroke and requires further study of its neuroprotective properties

Informe técnico final del proyecto “Manejo de desastres ante eventos meteorológicos extremos (sequías, heladas y lluvias intensas) como medida de adaptación ante el cambio climático en el valle del Mantaro - MAREMEX”

Resumen en inglés incluidoEl proyecto “Manejo de desastres ante eventos meteorológicos extremos (sequías, heladas y lluvias intensas) como medida de adaptación ante el cambio climático en el valle del Mantaro” - también conocido como MAREMEX-Mantaro -, se inició en febrero del año 2009, y con una duración de 36 meses tuvo por objetivo principal el de fortalecer la capacidad en el manejo del riesgo ante eventos meteorológicos extremos por parte tanto de la población como de las instituciones que tienen el manejo de los recursos naturales a su cargo, a fin de disminuir la vulnerabilidad de la población urbana y rural en el valle del Mantaro. El desarrollo del proyecto consideró la alta vulnerabilidad del valle del río Mantaro, - localizado en los Andes Centrales Peruanos -, a eventos meteorológicos extremos relacionados con la variabilidad climática, así como los estimados de que dicha vulnerabilidad se incrementaría en los siguientes años debido al cambio climático (IGP, 2005). Debido a la amplitud de la zona de estudio se priorizaron 3 subcuencas de estudio (Shullcas, Cunas y Achamayo), las que se escogieron tomando en cuenta varios factores: representatividad de ecosistemas, vulnerabilidad a la ocurrencia de los eventos meteorológicos identificados, accesibilidad, existencia de zonas urbanas de importancia, interés e intención de participar, etc. Entre los objetivos específicos se buscó fortalecer y profundizar los estudios sobre causas, ocurrencia e impactos de heladas, sequías y fenómenos de lluvias intensas en la región; identificar los actores claves involucrados y evaluar las actuales capacidades de los pobladores del valle del Mantaro en el manejo del riesgo de desastres ante la ocurrencia de eventos meteorológicos extremos; elaborar un plan integrado de manejo de riesgo y estrategias de adaptación frente a heladas, sequías y lluvias intensas en el valle del Mantaro (con la participación de autoridades locales, gobiernos regionales, comunidades, ONG y otros actores relevantes); y promover el fortalecimiento institucional y difusión de los resultados del proyecto a la población, instituciones y medios científicos, a través de la creación o fortalecimiento de capacidades de investigación de entidades e investigadores locales en temas de adaptación al cambio climático..