Synthesis of Diarylamines and Methylcarbazoles and Formal Total Synthesis of Alkaloids Ellipticine and Olivacine

En este documento se describe la síntesis química, vía microondas, de derivados de alcaloides elipticina y olivacina, así como su identificación espectroscópica inequívocas.New and efficient strategies for the conversion of 4-oxazolin-2-ones into 1-methyl and 1,4-dimethyl 3-formylcarbazoles are herein described. Highly convergent cascade and one-pot processes afforded the corresponding diarylamines, as in situ formed synthetic intermediates or final products in high overall yields. Special attention was given to the synthesis of methylated carbazoles by reacting 4,5-dimethyl-4-oxazolin-2-ones with enones under microwave irradiation. The carbazole scaffold was provided by the palladium(II)-catalyzed double C−H activation to generate oxidative cyclization of diarylamines. This methodology allowed for formal total syntheses of four naturally occurring pyrido[4,3-b]carbazole alkaloids ellipticine, 9-methoxyellipticine, olivacine, and 9-methoxyolivacine.Secretaría de Investigación y Estudios Avanzados de la UAEMex. CONACYT Ludwig K. Hellweg Foundation Secretaría de Investigación y Posgrado, del IP

Exploratory study on didactic aspects used in scientific-technical (STEM) dissemination conferences for students of secondary education

The connection between education and a country's economic and social development is unquestionable, and science and technology-related careers are of particular importance. Given the lack of vocations in these degrees, a number of mechanisms have been used to attract students, including science and technology conferences in secondary schools. Focusing on this type of lectures, this article aims to analyse the didactic aspects used by university lecturers who deliver this type of lectures. To this end, 16 teachers were interviewed using a structured interview. From the qualitative analysis of the interviews, we reached a series of results and conclusions, among which we would like to highlight the following: teachers see these lectures as a form of scientific dissemination which also helps to promote the degree courses they teach and serves as a support for attracting students; when choosing the content of the lecture, they mainly take into account the secondary school curriculum, including striking aspects and the results of their own research; the mediums used are mainly visual and supported by Do It Yourself techniques; the content is normally presented through presentations or practical laboratory exercises; finally, the documentation provided to students depends on the teacher giving the lecture, and there is no consensus on this pointPeer Reviewe

Recognition by familiarity is preserved in Parkinson's without dementia and Lewy-Body disease

Objective: The retrieval deficit hypothesis states that the lack of deficit in recognition often observed in patients with Parkinson's disease is because of the low retrieval requirements of the task, given that these patients have retrieval and not encoding deficits. To test this hypothesis we investigated recognition memory by familiarity in Parkinson’s patients and in patients with Lewy Bodies disease and Parkinson with dementia. Method: We analyzed to what extent the experimental groups were able to recognize by familiarity in a typical yes/no recognition memory task. The experimental groups were patients with early nondemented Parkinson’s disease, advanced nondemented Parkinson’s disease, demented Parkinson’s patients, and patients with dementia with Lewy Bodies. We compared their performance with a group of young and another group of old healthy participants. The estimation of familiarity was made by analyzing recognition of word targets and distractors consisting of combinations of different letters in comparison with a condition in which targets and distractors were composed of similar letters, even though subjects were unaware of the independent variable. Results: The results indicate that familiarity was used at the same level by controls, patients with early Parkinson’s disease and patients with dementia with Lewy Bodies. Although late Parkinson patients also used familiarity, its effect was only marginally significant. Patients with Parkinson’s disease and dementia were not capable of using familiarity in recognition memory. Conclusions: Our results support the retrieval deficit hypothesis as Parkinson’s patients without dementia show no deficit in a situation in which the retrieval requirements are minimal

Synthesis of 4,5,6,7-tetrahydrobenzoxazol-2-ones by a highly regioselective Diels-Alder cycloaddition of exo-oxazolidin-2-one dienes with chalcones

En este trabajo se describe la reactividad química de derivados de chalconas y dienos exo heterocíclicos, obteniéndose una serie de compuestos los cuales fueron caracterizados y rigurosamente identificados, demostrando de esta manera la conducta de estas moléculas en ambientes controlados.The synthesis of novel of 4,5,6,7-tetrahydrobenzoxazol-2-ones is herein reported. They were obtained in moderate to good yields by a highly regio- and stereoselective Diels-Alder cycloaddition of N-substituted exo-oxazolidin-2-one dienes with chalcones or bis-chalcones as dienophilesSecretaría de Investigación y Estudios Avanzados de la Universidad Autónoma del Estado de Méxic

Estimación del consumo hídrico de vid cv. Cabernet sauvignon mediante el modelo Shuttleworth y Wallace usando un vehículo aéreo no tripulado

37 p.Debido a la baja fracción de cobertura de viñedos conducidos en espaldera vertical simple, modelos como Penman-Monteith tienen problemas para estimar la evapotranspiración del cultivo, presentando diferencias importantes entre el valor estimado y el observado. Es por esto por lo que en este trabajo se utilizó el modelo de dos fuentes de Shuttleworth y Wallace (SW), complementado con información obtenida de un vehículo aéreo no tripulado (VANT), de tal manera de incorporar la variabilidad aportada por el suelo y el vigor del cultivo. Este trabajo se realizó en el valle de Pencahue, región del Maule, en un viñedo comercial de 6 años, conducido en espaldera vertical simple y con un sistema de riego por goteo. El modelo fue comparado con las mediciones obtenidas de un sistema de flujos turbulentos ubicado en el centro de la zona de estudio. Los indicadores utilizados para medir la correlación de ambos métodos fueron el cuadrado medio del error (RMSE), error medio absoluto (MAE) y el índice de acuerdo del modelo (d). Los resultados obtenidos indican que SW estimó con un RMSE de 34.16W m-1, 0.44mm día-1 y 0.14mm hora-1 el flujo de calor latente, la evapotranspiración diaria, y la evapotranspiración horaria, respectivamente. ABSTRACT: Due to the low coverture fraction of vineyards grow in simple vertical trellis, models like Penman-Monteith present problems in the estimation of actual evapotranspiration of the crop, showing important differences between the estimated and observed values. To solve this problem, this study uses the two-sources Shuttleworth and Wallace model (SW), which helped by aerial information obtained from an unmanned aerial vehicle (VANT), incorporates the spatial variability of the soil and the vineyard vigor. This work was made in Pencahue valley, Maule region, in a simple vertical trellis conducted six years-old vineyards with a drip irrigation system. SW was compared with the measures obtained from an Eddy Covariance system. The performance of the model was evaluated with the root mean square error (RMSE), mean absolute error (MAE) and the index of agreement of the model (d). results show that SW estimated with a RMSE of 34.16W m-1, 0.44mm day-1 and 0.14mm hour-1 the Latent heat flux, daily evapotranspiration and instant evapotranspiration, respectively

Enantiopure 4‐oxazolin‐2‐ones and 4‐methylene‐2‐oxazolidinones as chiral building blocks in a divergent asymmetric synthesis of heterocycles

En este trabajo se describe la reactividad de las oxazolidin-2-onas en un ambiente quiral obteniéndose resultados novedosos, los cuales se describen extensamente.Enantiopure 3‐((R)‐ and 3‐((S)‐1‐phenylethyl)‐4‐oxazoline‐2‐ones were evaluated as chiral building blocks for the divergent construction of heterocycles with stereogenic quaternary centers. The N‐(R)‐ or N‐(S)‐1‐phenylethyl group of these compounds proved to be an efficient chiral auxiliary for the asymmetric induction of the 4‐ and 5‐positions of the 4‐oxazolin‐2‐one ring through thermal and MW‐promoted nucleophilic conjugated addition to Michael acceptors and alkyl halides. The resulting adducts were transformed via a cascade process into fused six‐membered carbo‐ and heterocycles. The structure of the reaction products depended on the electrophiles and reaction conditions used. Alternative isomeric 4‐methylene‐2‐oxazolidinones served as chiral precursors for a versatile and divergent approach to highly substituted cyclic carbamates. DFT quantum calculations showed that the formation of bicyclic pyranyl compounds was generated by a diastereoselective concerted hetero‐Diels‐Alder cycloaddition.Instituto Politécnico Nacional, Secretaria de Investigación y Estudios Avanzados de la Universidad Autónoma del Estado de México, Universidad de Guanajuato y CONACYT

Pressurized Extraction as an Opportunity to Recover Antioxidants from Orange Peels: Heat treatment and Nanoemulsion Design for Modulating Oxidative Stress

Orange peel by-products generated in the food industry are an important source of value added compounds that can be potentially reused. In the current research, the effect of oven-drying (50–70 ◦C) and freeze-drying on the bioactive compounds and antioxidant potential from Navelina, Salustriana, and Sanguina peel waste was investigated using pressurized extraction (ASE). Sixty volatile components were identified by ASE-GC-MS. The levels of terpene derivatives (sesquitenenes, alcohols, aldehydes, hydrocarbons, and esters) remained practically unaffected among fresh and freeze-dried orange peels, whereas drying at 70 ◦C caused significative decreases in Navelina, Salustri ana, and Sanguina peels. Hesperidin and narirutin were the main flavonoids quantified by HPLC-MS. Freeze-dried Sanguina peels showed the highest levels of total-polyphenols (113.3 mg GAE·g −1 ), total flavonoids (39.0 mg QE·g −1 ), outstanding values of hesperedin (187.6 µg·g −1 ), phenol acids (16.54 mg·g −1 DW), and the greatest antioxidant values (DPPH•, FRAP, and ABTS•+ assays) in comparison with oven-dried samples and the other varieties. Nanotechnology approaches allowed the formulation of antioxidant-loaded nanoemulsions, stabilized with lecithin, starting from orange peel extracts. Those provided 70–80% of protection against oxidative UV-radiation, also decreasing the ROS levels into the Caco-2 cells. Overall, pressurized extracts from freeze-drying orange peel can be considered a good source of natural antioxidants that could be exploited in food applications for the development of new products of commercial interest

Herramientas para la evaluación multidimensional de uso para médicos de cuidados paliativos: proyecto ICO-Tool Kit

Introducción: el paciente y su familia presentan una serie de necesidades físicas, emocionales, sociales y espirituales que requieren ser evaluadas. Estas necesidades han de quedar registradas ya que han de permitir la fijación de objetivos asistenciales, la revisión de los resultados y su reevaluación posterior. La evaluación de estas necesidades con instrumentos comunes facilita la transmisión de la información entre los distintos profesionales sanitarios implicados en el proceso de atención. Objetivo: consensuar distintos instrumentos para una evaluación multidimensional en el paciente oncológico avanzado que deberían incluirse en cualquier valoración médica de equipo de cuidados paliativos de la red asistencial del Institut Català d'Oncologia. Material y método: técnica de consenso entre los distintos participantes mediante grupo de discusión. Acuerdo interobservador en grupo de discusión basado en la valoración tanto de la bibliografía existente sobre los instrumentos analizados, como de la experiencia práctica diaria de los miembros de los equipos en su empleo. El equipo de trabajo estuvo formado por una muestra representativa de los 3 centros participantes y constituida por 5 médicos, 4 psico-oncólogos y 4 trabajadores sociales. Todos con experiencia en cuidados paliativos y dedicación completa. De los distintos instrumentos analizados, se empleó para su valoración tanto la bibliografía existente de los mismos, así como la experiencia práctica de los equipos con su empleo. Se obtenía una puntuación y un grado de acuerdo que sirvió para la elección de los instrumentos que se consideraban más útiles y formarían parte del kit de evaluación. Resultado y conclusiones: tras discusión y análisis de los resultados, se seleccionaron los instrumentos que se consideraron más adecuados para la evaluación. Se definió un conjunto de instrumentos para la evaluación de las 3 dimensiones exploradas: física (antecedentes, estado funcional, dependencia, listado de síntomas y supervivencia), emocional (síntomas emocionales, incluyendo espiritualidad y cuidados al final de la vida) y social mostrando el porcentaje de acuerdo alcanzado para cada una de ellas

Bone Mass and the CAG and GGN Androgen Receptor Polymorphisms in Young Men

BACKGROUND: To determine whether androgen receptor (AR) CAG (polyglutamine) and GGN (polyglycine) polymorphisms influence bone mineral density (BMD), osteocalcin and free serum testosterone concentration in young men. METHODOLOGY/PRINCIPAL FINDINGS: Whole body, lumbar spine and femoral bone mineral content (BMC) and BMD, Dual X-ray Absorptiometry (DXA), AR repeat polymorphisms (PCR), osteocalcin and free testosterone (ELISA) were determined in 282 healthy men (28.6+/-7.6 years). Individuals were grouped as CAG short (CAG(S)) if harboring repeat lengths of < or = 21 or CAG long (CAG(L)) if CAG > 21, and GGN was considered short (GGN(S)) or long (GGN(L)) if GGN < or = 23 or > 23. There was an inverse association between logarithm of CAG and GGN length and Ward's Triangle BMC (r = -0.15 and -0.15, P<0.05, age and height adjusted). No associations between CAG or GGN repeat length and regional BMC or BMD were observed after adjusting for age. Whole body and regional BMC and BMD values were similar in men harboring CAG(S), CAG(L), GGN(S) or GGN(L) AR repeat polymorphisms. Men harboring the combination CAG(L)+GGN(L) had 6.3 and 4.4% higher lumbar spine BMC and BMD than men with the haplotype CAG(S)+GGN(S) (both P<0.05). Femoral neck BMD was 4.8% higher in the CAG(S)+GGN(S) compared with the CAG(L)+GGN(S) men (P<0.05). CAG(S), CAG(L), GGN(S), GGN(L) men had similar osteocalcin concentration as well as the four CAG-GGN haplotypes studied. CONCLUSION: AR polymorphisms have an influence on BMC and BMD in healthy adult humans, which cannot be explained through effects in osteoblastic activity