Facile synthesis of isoxazoles and pyrazoles from ß-diketohydrazones

Indexación: ScieloNew 3,5-dimethyl-4-[(E)-4-(R1-phenyl)diazenyl]isoxazoles and 3,5-dimethyl-1-(R2-phenyl)-4-[(E)-(R1-phenyl)diazenyl]-1H-pyrazoles may be obtained by reaction of 3-[2-(R1-phenyl)hydrazono)]pentane-2,4-dione with H2NOH-HCl and R2-4-C6H4-NHNH2, respectively. The reactions were performed in ethanol as solvent and catalyzed by glacial acetic acid.http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072009000300013&nrm=is

Exposure to hydrocarbons and chlorpyrifos alters the expression of nuclear receptors and antioxidant, detoxifying, and immune response proteins in the liver of the rainbow trout, Oncorhynchus mykiss

The development of oil and gas production together with the fruit production in nearby areas of North Patagonia, Argentina, suggests aquatic pollution scenarios which include permanent oil pollution combined with short events of pesticides application. It has been reported that oil hydrocarbons activate the aryl hydrocarbon receptor (AhR) pathway in the rainbow trout, Oncorhynchus mykiss, and that the insecticide Chlorpyrifos (CPF) interacts with these effects. Thus, it is interesting to investigate whether hydrocarbons and insecticides, applied by separate or combined, can affect fish health and reproductive signaling by acting on different nuclear receptors’ regulatory pathways. To study this kind of interactions, we exposed juvenile rainbow trout to water accommodated fraction (WAF) of crude oil (62 μg L−1 TPH) for 48 h and subsequently exposed the livers ex vivo to the insecticide Chlorpyrifos (CPF) (20 µg L−1) for 1 h. We analyzed the mRNA expression of nuclear receptors and proteins involved in detoxifying, antioxidant, immune and apoptosis responses by qRT−PCR. We also performed histopathological analysis. WAF induced the expression of the androgen (AR) and the Liver X receptor (LXR) by 8- and 3-fold, respectively. AR induction was reversed by subsequent exposure to CPF. The progesterone receptor (PR) and glucocorticoid receptor (GR) were increased 2-fold and 3-fold by WAF respectively, while estrogen and mineralocorticoid receptors were not affected. GR was also induced by CPF with an additive effect in the WAF−CPF treatment. The antioxidant genes, gamma glutamyl transferase (GGT), superoxide dismutase (SOD1) were induced by WAF (2–3-fold). WAF upregulated the ATP Binding Cassette Subfamily C Member 2 (ABCC2, MRP2) (4-fold) and downregulated alkaline phosphatase. WAF also induced the inflammatory interleukins (IL) IL-8, and IL-6 and the anti-inflammatory IL-10, while CPF induced the inflammatory tumor necrosis factor (-α) and IL-6, and activated the intrinsic apoptotic pathway through the induction of caspases 3 and 9. Both, WAF and CPF downregulated the expression of the extrinsic apoptosis initiator caspase 8 and the inflammatory caspase 1. In conclusion, WAF hydrocarbons alter O. mykiss endocrine regulation by inducing AR, PR and GR. The subsequent exposure to CPF reverses AR, suggesting a complex interaction of different pollutants in contaminated environments, WAF hydrocarbons alter liver metabolism by inducing the expression of LXR, GR, antioxidant and detoxifying enzymes, and both inflammatory and anti-inflammatory cytokines, and causing mild hepatic steatosis. CPF activates inflammatory and stress responses associated with the induction of inflammatory cytokines together with apoptosis initiator and executioner caspases.Fil: de Anna, Julieta Soledad. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Centro Cientifico Tecnologico Conicet - Patagonia Norte. Instituto de Investigaciones En Biodiversidad y Medioambiente. Subsede Junín de Los Andes-inibioma-centro de Ecología Aplicada del Neuquén (cean) | Universidad Nacional del Comahue. Centro Regional Universitario Bariloche. Instituto de Investigaciones En Biodiversidad y Medioambiente. Subsede Junín de Los Andes-inibioma-centro de Ecología Aplicada del Neuquén (cean).; ArgentinaFil: Castro, Juan Manuel. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Centro Cientifico Tecnologico Conicet - Patagonia Norte. Instituto de Investigaciones En Biodiversidad y Medioambiente. Subsede Junín de Los Andes-inibioma-centro de Ecología Aplicada del Neuquén (cean) | Universidad Nacional del Comahue. Centro Regional Universitario Bariloche. Instituto de Investigaciones En Biodiversidad y Medioambiente. Subsede Junín de Los Andes-inibioma-centro de Ecología Aplicada del Neuquén (cean).; ArgentinaFil: Arias Darraz, Luis. Universidad Austral de Chile; ChileFil: Elías, Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Patagonia Norte; Argentina. Comisión Nacional de Energía Atómica. Centro Atómico Bariloche; ArgentinaFil: Cárcamo, Juan Guillermo. Universidad Austral de Chile; Chile. Interdisciplinary Center for Aquaculture Research; ChileFil: Luquet, Carlos Marcelo. Consejo Nacional de Investigaciones Cientificas y Tecnicas. Centro Cientifico Tecnologico Conicet - Patagonia Norte. Instituto de Investigaciones En Biodiversidad y Medioambiente. Subsede Junín de Los Andes-inibioma-centro de Ecología Aplicada del Neuquén (cean) | Universidad Nacional del Comahue. Centro Regional Universitario Bariloche. Instituto de Investigaciones En Biodiversidad y Medioambiente. Subsede Junín de Los Andes-inibioma-centro de Ecología Aplicada del Neuquén (cean).; Argentin

2-[2-(4-Acetyl­phen­yl)hydrazinyl­idene]-1,3-diphenyl­propane-1,3-dione

In the title compound, C23H18N2O3, the inter­planar angle between the benzoyl units is 80.51 (6)° while the dihedral angles between the hydrazinyl­idene and benzoyl groups are 43.43 (6) and 54.16 (6)°. In the crystal, a strong resonance-assisted intra­molecular N—H⋯O hydrogen bond is observed. The mol­ecules form an inversion dimer via a pair of weak C—H⋯O hydrogen bonds and a π–π inter­action [centroid–centroid distance of 3.5719 (10) Å]. These dimers are linked via weak C—H⋯O contacts, forming chains along the b axis

Identificación de blancos terapéuticos putativos en Caligus rogercresseyi utilizando bases de datos de transcriptómica del parásito

86 p.Caligus rogercresseyi es un ectoparásito que afecta en gran medida la producción de salmónidos en Chile. Se estima que las pérdidas directas e indirectas asociadas a Caligus en el año 2013 fueron de alrededor de US$80 millones. De la misma manera, los costos para la industria desde los primeros brotes de Caligus resistente a los medicamentos en 2007 ascendieron a US$ 700 millones, lo que indica la gran importancia de estudiar mecanismos de control de este parásito. En la actualidad se ha experimentado un evidente desarrollo de resistencias de C. rogercresseyi frente a los distintos tratamientos aplicados. Dentro de los principales factores que influyeron en esta pérdida de eficacia (resistencia) se menciona el uso exclusivo y continuado del producto por más de 7 años. Para este trabajo contamos con un set de datos transcriptómicos del parasito, es decir, secuencias obtenidas a partir de RNA. Las ventajas que tiene analizar el RNA o transcriptoma de un organismo, es el poder identificar cambios de expresión génica en determinado momento celular de un tratamiento, con respecto a un control, es decir, obtenemos una imagen temporal del panorama celular asociado a los RNAs, con respecto al panorama del tratamiento, haciendo comparables y evaluables los niveles de expresión en ambas condiciones mediante algoritmos estadísticos. En este contexto, la bioinformática juega un papel fundamental, como una disciplina integrativa que se ha convertido en un componente intrínseco en esta nueva fase de estudios moleculares a gran escala, pues provee herramientas para el manejo, análisis y manipulación de grandes cantidades de datos. Durante los últimos años, se ha logrado obtener información del RNA de variados organismos, los cuales son sujetos de investigación. Es por esto que técnicas de secuenciación de RNA (bajo el protocolo de secuenciación RNA-seq) han demostrado ser una herramienta de gran alcance y con una gama muy diversa de aplicaciones. Con respecto a éste trabajo de memoria de título, el objetivo principal se basa en identificar secuencias aminoacídicas deducidas, asociadas a posibles proteínas o péptidos vinculados con resistencia farmacológica y/o como blancos terapéuticos putativos a través del análisis de las bases de datos transcriptómicas de Caligus rogercresseyi. Para lograr lo anterior, se realizó un análisis de las bases de datos transcriptómicas de Caligus rogercresseyi a partir de un ensamble de novo del transcriptoma del parásito, para luego lograr identificar a través de expresión diferencial los distintos niveles de expresión existentes con tratamientos de Emamectina y Deltametrina en C.rogercresseyi. Se utilizó un protocolo de RNA-seq, en conjunto con otras herramientas bioinformáticas, con las cuales se buscó encontrar blancos terapéuticos putativos, que permitan desarrollar futuros estudios para combatir con éxito a este parásito y, de esta manera a largo plazo, lograr disminuir de las pérdidas económicas causadas por Caligus. Y desde otra perspectiva, que en ningún caso es menos importante, la generación de este conocimiento posibilitará contribuir en una posible disminución de la contaminación ambiental asociada a los tratamientos químicos, como los realizados hoy en día./ ABSTRACT: Caligus rogercresseyi is an ectoparasite that greatly affects the production of salmonids in Chile. It is estimated that the direct and indirect losses associated with sea lice in 2013 were about US $80 millions. Similarly, the costs for the industry since the first outbreaks of drug-resistant sea lice in 2007 amounted to US$ 700 million, which indicates the great importance of studying mechanisms controlling this pest. Today it has experienced an obvious development of resistance of C. rogercresseyi against the various treatments applied. Among the main factors influencing this efficiency loss (resistance) mentioned the exclusive and continuous use of the product for more than 7 years.For this study we have a set of the parasite transcriptome data, that is to say sequences obtained from RNA. The advantages analyze the RNA or transcriptome of an organism, in order to identify gene expression changes in certain cells during a treatment, with respect to control, that is to say, obtain a temporary image cell panorama of associated RNAs, with respect to the treatment panorama, making comparable and evaluable expression levels in both conditions using statistical algorithms. In this context, bioinformatics plays a key role as an integrative discipline that has become an intrinsic component in this new phase of molecular-scale studies, it provides tools for operation, analysis and handling of large amounts of data. In recent years, it has been possible to obtain information of various organisms RNA, which are subject to research. That is why RNA sequencing techniques (under the protocol sequencing RNA-seq) have proven to be a powerful tool with a very diverse range of applications. With respect to this thesis, the main objective is based on identifying amino acid sequences deduced, associated with possible proteins or peptides associated with drug resistance and / or as therapeutic targets putative through the analysis of the basis of transcriptomic data Caligus rogercresseyi. To achieve this, an analysis of the basis of transcriptomic data Caligus rogercresseyi was performed from an ensemble de novo transcriptome parasite, and then be able to identify through differential expressions, different levels of existing expression treatments Emamectin and deltamethrin in C. rogercresseyi. IX A protocol of RNA-seq was used in conjunction with other bioinformatics tools, with which they seek to find putative therapeutic targets, in order to develop future studies to successfully combat this parasite and thus long-term, achieve the decrease of economic losses caused by sea lice. And from another perspective, that in no case is less important, the generation of this knowledge will enable a contribution to a possible reduction of environmental pollution associated with chemical treatments, such as those made today

Gills CYP1A of Oncorhynchus mykiss as a sensitive biomarker of crude oil pollution in freshwater environments

The induction of CYP1A activity (EROD) and protein expression was compared in liver and gills of rainbow trout from a stream polluted with crude oil, and through laboratory exposures to 1% and 5% of water accommodated fraction of the crude oil (WAF) for 1 and 4 days. Gills EROD increased 1.6–2.7-fold in fish from the polluted stream and during experiments, while liver EROD was induced only by 1% WAF at day 1 (1.5-fold). Contrastingly, crude oil pollution strongly induced both liver and gills CYP1A protein expression in the field (14-36-fold) and in experiments (4-25-fold). This highlights that crude oil induced CYP1A activity markedly in gills but only slightly or not at all in the liver, suggesting that differences between organ EROD activities are related to the modulation of CYP1A enzyme activity but not to the regulation at transcriptional or translational levels.Fil: Leggieri, Leonardo Ramón. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Patagonia Norte. Instituto de Investigaciones en Biodiversidad y Medioambiente. Universidad Nacional del Comahue. Centro Regional Universidad Bariloche. Instituto de Investigaciones en Biodiversidad y Medioambiente; ArgentinaFil: de Anna, Julieta Soledad. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Patagonia Norte. Instituto de Investigaciones en Biodiversidad y Medioambiente. Universidad Nacional del Comahue. Centro Regional Universidad Bariloche. Instituto de Investigaciones en Biodiversidad y Medioambiente; ArgentinaFil: Cárcamo, Juan Guillermo. Centro Interdisciplinario para la Investigación Acuícola; Chile. Universidad Austral de Chile; ChileFil: Cerón, Gerardo Abel. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Comahue. Centro Regional Universidad Bariloche. Departamento de Zoología; ArgentinaFil: Darraz, Luis Arias. Universidad Austral de Chile; ChileFil: Panebianco, Antonella. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Patagonia Norte. Instituto de Investigaciones en Biodiversidad y Medioambiente. Universidad Nacional del Comahue. Centro Regional Universidad Bariloche. Instituto de Investigaciones en Biodiversidad y Medioambiente; ArgentinaFil: Luquet, Carlos Marcelo. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Patagonia Norte. Instituto de Investigaciones en Biodiversidad y Medioambiente. Universidad Nacional del Comahue. Centro Regional Universidad Bariloche. Instituto de Investigaciones en Biodiversidad y Medioambiente; Argentin

A second monoclinic polymorph of 2-[2-(4-meth­oxy­phen­yl)hydrazinyl­idene]-1,3-diphenyl­propane-1,3-dione

The title compound, C22H18N2O3 is the second monoclinic polymorph (P21/c) of the compound, the first being reported in space group P21 [Bertolasi et al. (1993 ▶). J. Chem. Soc. Perkin Trans. 2, pp. 2223–2228]. In the mol­ecular structure of the title compound, the inter­planar angle between the benzoyl units is 80.04 (5)°, while the corresponding angles between the phenyl­hydrazinyl­idene and benzoyl groups are 36.11 (5) and 55.77 (2)°. A strong resonance-assisted intra­molecular N—H⋯O hydrogen bond is found. In the crystal, the entire supra­molecular structure is constructed by weak inter­molecular C—H⋯O inter­actions and an inter-ring π–π inter­action [centroid–centroid distance = 3.6088 (8) Å]

2-[2-(3-Chloro­phen­yl)hydrazinyl­idene]-1,3-diphenyl­propane-1,3-dione

The mol­ecular structure of the title compound, C21H15ClN2O2, features one strong intra­molecular N—H⋯O resonance-assisted hydrogen bond (RAHB). In the crystal, mol­ecules form inversion-related dimers via pairs of weak inter­molecular N—H⋯O contacts. These dimers are further stabilized via three weak C—H⋯O contacts, developing the three-dimensional structure

Risk and outcomes of COVID-19 in patients with multiple sclerosis

Background and purpose Limited information is available on incidence and outcomes of COVID-19 in patients with multiple sclerosis (MS). This study investigated the risks of SARS-CoV-2 infection and COVID-19-related outcomes in patients with MS, and compared these with the general population. Methods A regional registry was created to collect data on incidence, hospitalization rates, intensive care unit admission, and death in patients with MS and COVID-19. National government outcomes and seroprevalence data were used for comparison. The study was conducted at 14 specialist MS treatment centers in Madrid, Spain, between February and May 2020. Results Two-hundred nineteen patients were included in the registry, 51 of whom were hospitalized with COVID-19. The mean age ± standard deviation was 45.3 ± 12.4 years, and the mean duration of MS was 11.9 ± 8.9 years. The infection incidence rate was lower in patients with MS than the general population (adjusted incidence rate ratio = 0.78, 95% confidence interval [CI] = 0.70–0.80), but hospitalization rates were higher (relative risk = 5.03, 95% CI = 3.76–6.62). Disease severity was generally low, with only one admission to an intensive care unit and five deaths. Males with MS had higher incidence rates and risk of hospitalization than females. No association was found between the use of any disease-modifying treatment and hospitalization risk. Conclusions Patients with MS do not appear to have greater risks of SARS-CoV-2 infection or severe COVID-19 outcomes compared with the general population. The decision to start or continue disease-modifying treatment should be based on a careful risk–benefit assessment.post-print996 K

Gestión del conocimiento: perspectiva multidisciplinaria. Volumen 11

El libro “Gestión del Conocimiento. Perspectiva Multidisciplinaria”, Volumen 11, de la Colección Unión Global, es resultado de investigaciones. Los capítulos del libro, son resultados de investigaciones desarrolladas por sus autores. El libro cuenta con el apoyo de los grupos de investigación: Universidad Sur del Lago “Jesús María Semprúm” (UNESUR), Zulia – Venezuela; Universidad Politécnica Territorial de Falcón Alonso Gamero (UPTAG), Falcón – Venezuela; Universidad Politécnica Territorial de Mérida Kleber Ramírez (UPTM), Mérida – Venezuela; Universidad Guanajuato (UG) - Campus Celaya - Salvatierra - Cuerpo Académico de Biodesarrollo y Bioeconomía en las Organizaciones y Políticas Públicas (C.A.B.B.O.P.P), Guanajuato – México; Centro de Altos Estudios de Venezuela (CEALEVE), Zulia – Venezuela, Centro Integral de Formación Educativa Especializada del Sur (CIFE - SUR) - Zulia - Venezuela, Centro de Investigaciones Internacionales SAS (CIN), Antioquia - Colombia.y diferentes grupos de investigación del ámbito nacional e internacional que hoy se unen para estrechar vínculos investigativos, para que sus aportes científicos formen parte de los libros que se publiquen en formatos digital e impreso

P-glycoprotein expression and pharmacological modulation in larval stages of Echinococcus granulosus

P-glycoprotein (Pgp) is an ATP-dependent transporter involved in the efflux of a wide variety of lipophilic substrates, such as toxins and xenobiotics, out of cells. Pgp expression level is associated with the ineffective therapeutic treatment of cancer cells and microbial pathogens which gives it high clinical importance. Research on these transporters in helminths is limited. This work describes for the first time the Echinococcus granulosus Pgp (Eg-Pgp) expression, in a model cestode parasite and an important human pathogen. Based on calcein efflux assays in the presence of common Pgp modulators, we demonstrated the occurrence of active Eg-Pgp in protoscoleces and metacestodes. Eg-Pgp, which showed a molecular mass of ~130 kDa in western blots, is localized in the suckers and the tegument of control protoscoleces as well as in the subtegument or all parenchymatous cells of protoscoleces treated with Pgp-interfering agents. We also identified five genes encoding Pgp which are constitutively expressed in protoscoleces and metacestodes. We showed that the Eg-pgp1 and Eg-pgp2 transcripts were up-regulated in response to in vitro drug treatment with amiodarone and loperamide, in agreement with the increased polypeptide levels. Finally, in vitro treatment of protoscoleces and metacestodes with trifluoperazine and loperamide was lethal to the parasites. This indicates that both drugs as well as cyclosporine A negatively modulate the E. granulosus Pgp efflux activity, favoring the retention of these drugs in the larval tissue. These events could be associated with the reduction in protoscolex and metacestode viability.Fil: Nicolao, María Celeste. Universidad Nacional de Mar del Plata. Facultad de Ciencias Exactas y Naturales. Departamento de Biologia. Laboratorio de Zoonosis Parasitarias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Denegri, Guillermo Maria. Universidad Nacional de Mar del Plata. Facultad de Ciencias Exactas y Naturales. Departamento de Biologia. Laboratorio de Zoonosis Parasitarias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Cárcamo, Juan Guillermo. Universidad Austral de Chile.; ChileFil: Cumino, Andrea Carina. Universidad Nacional de Mar del Plata. Facultad de Ciencias Exactas y Naturales. Departamento de Biologia. Laboratorio de Zoonosis Parasitarias; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional de Mar del Plata. Facultad de Ciencias Exactas y Naturales. Departamento de Química; Argentin