Diseño mecánico de los elementos de transmisión de un aerogenerador de 1, 3 MW

Partiendo de la potencia que ha de generar se pretende realizar el diseño de los distintos elementos de transmisión de un aerogenerador con el fin de garantizar un funcionamiento óptimo del mismo.

American plants. : v. 1-3; Jan. 1907-[1910].

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Synthesis and antibacterial study of some s-substituted aliphatic analogues of 2-mercapto-5-(1-(4-toluenesulfonyl) piperidin-4-yl)-1,3,4-oxadiazole

Purpose: To synthesize a series of analogues of 1,3,4-oxadiazole and to evaluate their antibacterial activity. Methods: Ethyl piperidin-4-carboxylate (1) was mixed with 4-toluenesulfonyl chloride (2) in benignant conditions to yield ethyl 1-(4-toluenesulfonyl)piperidin-4-carboxylate (3) and then 1-(4- toluenesulfonyl)piperidin-4-carbohydrazide (4). Intermolecular cyclization of 4 into 2-mercapto-5-(1-(4- toluenesulfonyl) piperidin-4-yl)-1,3,4-oxadiazole (5) was obtained on reflux with CS2 in the presence of KOH. Molecule 5 was stirred with alkyl halides, 6a-i, in DMF in the presence of LiH to synthesize the final compounds, 7a-i. The structures of these molecules were elucidated by Fourier transform infra-red (FTIR) spectroscopy, proton nuclear magnetic resonance (1H-NMR) and electron impact mass spectrometry (EI-MS). Antibacterial activity was evaluated against five bacterial strains, namely, Salmonella typhi, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis, with ciprofloxacin used as standard antibacterial agent. Results: Out of nine synthesized derivatives, compound 7a was the most active against three bacterial strains, S. typhi, E. coli and P. aeruginosa, with minimum inhibitory concentration (MIC) of 9.11 ± 0.40, 9.89 ± 0.45 and 9.14 ± 0.72 μM, respectively, compared with 7.45 ± 0.58, 7.16 ± 0.58 and 7.14 ± 0.18 μM, respectively, for the reference standard (ciprofloxacin). Similarly, compounds 7a - 7c showed relatively good antibacterial activity against B. subtilis strain while compound 7e - 7g revealed good results against S. typhi bacterial strain. Conclusion: The results indicate that S-substituted derivatives of the parent compound are more effective antibacterial agents than the parent compound, even with minor differences in substituents

Preliminary structure-activity relationship studies on some novel s-substituted aliphatic analogues of 5-{1-[(4- chlorophenyl) sulfonyl]-3-piperidinyl}-1, 3, 4-oxadiazol-2-yl sulfide

Purpose: To study the structure-activity relationships of synthetic multifunctional sulfides through evaluation of lipoxygenase and anti-bacterial activities. Methods: S-substituted derivatives of the parent compound 5-(1-(4-chlorophenylsulfonyl) piperidin-3- yl)-1, 3, 4-oxadiazole-2-thiol were synthesized through reaction with different saturated and unsaturated alkyl halides in DMF medium, with NaH catalyst. Spectral characterization of each derivative was carried out with respect to IR, 1H - NMR, 13C - NMR and EI - MS. The lipoxygenase inhibitory and antibacterial activities of the derivatives were determined using standard procedures. Results: Compound 5e exhibited higher lipoxygenase inhibitory potential than the standard (Baicalein®), with % inhibition of 94.71 ± 0.45 and IC50 of 20.72 ± 0.34 μmoles/L. Compound 5b showed significant antibacterial potential against all the bacterial strains with % inhibition ranging from 62.04 ± 2.78, 69.49 ± 0.41, 63.38 ± 1.97 and 59.70 ± 3.70 to 78.32 ± 0.41, while MIC ranged from 8.18 ± 2.00, 10.60 ± 1.83, 10.84 ± 3.00, 9.81 ± 1.86 and 11.73 ± 5.00 μmoles/L for S. typhi, E. coli, P. aeruginosa, B. subtilis and S. aureus, respectively. Compounds 5d, 5e and 5g showed good antibacterial activity against S. typhi and B. subtilis bacterial strains. Conclusion: The results suggest that compound 5e bearing n-pentyl group is a potent lipoxygenase inhibitor, while compound 5b with n-propyl substitution is a strong antibacterial agent. In addition, compounds 5d, 5e and 5g bearing n-butyl, n-pentyl and n-octyl groups, respectively, are good antibacterial agents against S. typhi and B. subtilis.

S-Alkylated/aralkylated 2-(1H-indol-3-yl-methyl)-1,3,4- oxadiazole-5-thiol derivatives. 1. Synthesis and characterization

Purpose: To synthesize and characterize S-alkylated/aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4- oxadiazole-5-thiol derivatives. Methods: 2-(1H-indol-3-yl)acetic acid (1) was reacted with absolute ethanol and catalytic amount of sulfuric acid to form ethyl 2-(1H-indol-3-yl)acetate (2) which was transformed to 2-(1H-indol-3- yl)acetohydrazide (3) by refluxing with hydrazine hydrate in methanol. Ring closure reaction of 3 with carbon disulfide and ethanolic potassium hydroxide yielded 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5- thiol (4) which was finally treated with alkyl/aralkyl halides (5a-u) in DMF and NaH to yield Salkylated/ aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiols (6a-u). Structural elucidation was done by IR, 1H-NMR and EI-MS techniques Results: 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol (4) was synthesized as the parent molecule and was characterized by IR and the spectrum showed peaks resonating at (cm-1) 2925 (Ar-H), 2250 (S-H ), 1593 (C=N ) and 1527 (Ar C=C ); 1H-NMR spectrum showed signals at δ 11.00 (s, 1H, NH-1ʹ), 7.49 ( br.d, J = 7.6 Hz, 1H, H-4\'), 7.37 (br.d, J = 8.0 Hz, 1H, H-7\'), 7.34 (br.s, 1H, H-2\'), 7.09 (t, J = 7.6 Hz, 1H, H-5\'), 7.00 (t, J = 7.6 Hz, 1H, H-6\') and 4.20 (s, 2H, CH2-10ʹ). EI-MS presented different fragments peaks at m/z 233 (C11H9N3OS)˙+ [M+2]+, 231 (C11H9N3OS)˙+ [M]+, 158 (C10H8NO)+, 156 (C10H8N2)˙+, 130 (C9H8N)+. The derivatives (6a-6u) were prepared and characterized accordingly. Conclusion: S-alkylated/aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiols (6a-u) were successfully synthesized.

S-Alkylated/aralkylated 2-(1H-indol-3-yl-methyl)-1,3,4- oxadiazole-5-thiol derivatives. 2. Anti-bacterial, enzymeinhibitory and hemolytic activities

Purpose: To evaluate the antibacterial, enzyme-inhibitory and hemolytic activities of Salkylated/ aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol derivatives. Methods: Antibacterial activities of the compounds were evaluated using broth dilution method in 96 well plates. Enzyme inhibitory activities assays were investigated against α-glucosidase, butyrylcholinesterase (BchE) and lipoxygenase (LOX) using acarbose, eserine and baicalien as reference standards, respectively. A mixture of enzyme, test compound and the substrate was incubated and variation in absorbance noted before and after incubation. In tests for hemolytic activities, the compounds were incubated with red blood cells and variations in absorbance were used as indices their hemolytic activities. Results: The compounds were potent antibacterial agents. Five of them exhibited very good antibacterial potential similar to ciprofloxacin, and had minimum inhibitory concentrations (MIC) of at least 9.00 ± 4.12 μM against S. aureus, E.coli, and B. subtilis. One of the compounds had strong enzyme inhibitory potential against α-glucosidase, with IC50 of 17.11 ± 0.02 μg/mL which was better than that of standard acarbose (IC50 38.25 ± 0.12 μg/mL). Another compound had 1.5 % hemolytic activity. Conclusion: S-Alkylated/aralkylated 2-(1H-indol-3-ylmethyl)-1,3,4-oxadiazole-5-thiol deviratives with valuable antibacterial, anti-enzymatic and hemolytic activities have been successfully synthesized. These compounds may be useful in the development of pharmaceutical products.

Theory and optimisation of 1.3 and 1.55 μm (Al)InGaAs metamorphic quantum well lasers

The use of InGaAs metamorphic buffer layers (MBLs) to facilitate the growth of lattice-mismatched heterostructures constitutes an attractive approach to developing long-wavelength semiconductor lasers on GaAs substrates, since they offer the improved carrier and optical confinement associated with GaAs-based materials. We present a theoretical study of GaAs-based 1.3 and 1.55 μm (Al)InGaAs quantum well (QW) lasers grown on InGaAs MBLs. We demonstrate that optimised 1.3 μm metamorphic devices offer low threshold current densities and high differential gain, which compare favourably with InP-based devices. Overall, our analysis highlights and quantifies the potential of metamorphic QWs for the development of GaAs-based long-wavelength semiconductor lasers, and also provides guidelines for the design of optimised devices.

Bland rutschbanebrallor och halkiga stockar : En studie om hur förskollärare tillsammans med barnen arbetar utomhus med fysikaliska begrepp som återkommer i läroplanen för åk 1-3.

The purpose of this study was to find out if preschool teachers use physical concepts included in thecurriculum for grade 1-3 (gravity, center of gravity, equilibrium, balance and friction) with the children in the outdoor environment at the preschool, if preschool teachers believe it is concepts that works to use with children in preschool outdoor environment and if the work could be developed regarding these physical concepts. To conduct the study, observations were done of preschool yards and semi-structured interviewswere conducted with preschool teachers who work in preschool right now. The result shows that it requires little resources to work with these concepts outdoors and teachers are positive to use the concepts but they do not use it to the extent they would like for a variety of reasons. In various ways, the preschool teachers also expresses that it is possible for children to absorb the physical concepts at preschool and it would help to later build a foundation in the form of childrens thinking that science is something fun and exciting that belong in their everyday lives.

Undervisningsmetoder inom läsförståelse i teori och praktik. : Sex lärares uppfattningar och konkreta arbete gällande undervisningen inom läsförståelse i årskurs 1-3.

Resultaten av de internationella undersökningarna PISA 2011 och PIRLS 2011 visar att de svenska elevernas resultat inom läsförståelse försämrats. I Skolinspektionen granskning framkommer det att diskussioner och textsamtal har en relativt liten del av undervisningen av läsförståelse i Sverige idag. Tidigare forskning har ringat in fyra metoder som anses effektivast för elevers utveckling av läsförståelse. Textsamtal, diskussioner och reflektioner har avgörande roller inom alla fyra undervisningsmetoder. Syftet med denna studie är att synliggöra hur sex lärare tänker kring, samt konkret arbetar med, undervisningen av läsförståelse, för att se om de fyra metoderna går att återfinna i de sex lärarnas undervisning. Metoderna som används är semistrukturerade intervjuer samt strukturerade observationer. Resultatet av studien visar att den strategiinriktade undervisningen dominerar undervisningen bland de sex lärarna, och att innehållsorienterad undervisning, vilken visats effektivast i forskningen, är ytterst begränsad. Samtidigt beskriver samtliga lärare att samtal och diskussioner bör vara en stor del av undervisningen inom läsförståelse. En slutsats av studien är att synen på undervisningen av läsförståelse varierar mellan de sex lärarna, samt att allt undervisningsmaterial är baserat på läsförståelsestrategier. Dock förekommer knappt diskussioner och samtal i samband med undervisningen av strategier, vilket är en viktig del för att arbetet med strategiinriktad undervisning ska kunna utveckla elevernas läsförståelse på bästa sätt.

Lärares syfte med laborativt arbete i NOundervisningen i årskurs 1-3 : En kvalitativ intervjustudie om sex lärares syfte med laborativt arbete i NO-undervisningen

Syftet med denna kvalitativa studie var att undersöka lärares syfte med laborativt arbete i årskurs 1-3 i NO-undervisningen samt vilka svårigheter som lärarna beskriver med det laborativa arbetssättet i NO-undervisningen. Studien har genomförts med hjälp av kvalitativa intervjuer av sex lärare som är verksamma i årskurserna 1-3. Alla tre årskurserna finns representerade i studien. De resultat som framkommit i studien är att lärare har flera olika syftet med det laborativa arbetet i NO-undervisningen. De syften som framkom var att öka förståelsen för naturvetenskapliga fenomen hos eleverna, öka elevernas motivation och intresse för naturvetenskap, erbjuda elever att uppleva naturvetenskap med händerna, erbjuda eleverna en möjlighet att träna på läroplanens mål, erbjuda eleverna en undervisning som utgår från varje elevs förutsättningar. Studiens frågeställningar berör även hur de intervjuade lärarna använder sig av laborativt arbete samt vilka svårigheter som lärarna uppger finnas med arbetssättet. Studien visar då att lärarna främst arbetar laborativt utomhus främst med biologi och att den svårigheten som flest lärare påpekade var avsaknaden av material.

Síntese selectiva de moléculas com potencial interesse biológico. Desenvolvimento de metodologias sustentáveis

Dissertação apresentada para obtenção do Grau de Doutor em Química Sustentável pela Universidade Nova de Lisboa, Faculdade de Ciências e Tecnologia

Síntesis y propiedades fisicoquímicas de estructuras moleculares fotoactivas derivadas de macrociclos tetrapirrólicos y fullereno C60

En el presente plan se diseñaran y sintetizaran nuevas estructuras moleculares derivadas de macrociclos tetrapirrólicos y fullereno C60. Posteriormente, se evaluarán sus propiedades fisicoquímicas y fotodinámicas con el fin de utilizarlos como fotosensibilizadores en la inactivación fotodinámica (PDI) de microorganismos. La síntesis de porfirinas se realizará por la condensación de dipirrometanos, sustituidos en la posición meso, con una mezcla binaria de benzaldehídos catalizada por ácido. Los grupos sustituyentes serán seleccionados de acuerdo a las características del macrociclo pirrólico que se desee obtener. Otra familia de compuestos con propiedades interesantes como fotosensibilizadores son los derivados de fullereno C60, los cuales serán sintetizados mediante la cicloadición 1,3-dipolar entre la función aldehído del sustituyente elegido y el fullereno C60, en presencia de N-metilglicina.Una alternativa interesante de nuevos compuestos para ser evaluados como agentes fotodinámicos son las díadas constituidas por estructuras con diferentes características dadora y aceptora de electrones, tal como porfirina-C60. Estas macromoléculas, son capaces de formar estados de separación de carga fotoinducido, lo que permite no sólo inactivar microorganismos en presencia de oxígeno, sino también en condiciones anóxicas dependiendo del microentorno en el cual se encuentre. La actividad fotodinámica de los nuevos agentes fototerapéuticos será evaluada medios homogéneos y en sistemas microheterogéneos, tales como micelas y ciclodextrinas conteniendo sustratos biológicamente activos. Estos estudios permitirán seleccionar los posibles sensibilizadores para ser aplicados en la PDI. Por lo tanto, el proyecto propone la acción combinada de un fotosensibilizador efectivo, activado por la luz visible en el medio biológico, para producir especies reactivas de oxígeno, las cuales causan un efecto citotóxico que conduce a la muerte celular.

Cycloadditions of chiral carbonyl ylides with imine dipolarophiles as a route to enantiomerically pure alpha-amino-beta-hydroxy acids

The preparation of enantiomerically pure threo-beta-amino-alpha-hydroxy acids via 1,3-dipolar cycloadditions of imine dipolarophiles with the chiral isomunchnone derived from (5R)-5-phenylmorpholin-3-one 1 is described. The cycloadducts were obtained with excellent diastereofacial- and exo-selectivity. Subsequent hydrolysis and chemoselective exocyclic amide cleavage afforded the threo-beta-amino-alpha-hydroxy acids with recovery of the initial chiral auxiliary. (C) 2009 Published by Elsevier Ltd.

Synthese und Charakterisierung zylindrischer Poly(2-oxazolin)bürsten als Nanocarrier für Drug Delivery Systeme

Inspiriert durch natürlich vorkommende Peptide, sind Poly(2-oxazoline) vielversprechende Kandidaten für Anwendungen in Bereichen des kontrollierten Wirkstoff- bzw. Gentransportes, wie die moderne Biomedizin dies fordert. Da Polyoxazoline als strukturisomere Amide von natürlichen Polypeptiden aufgefasst werden können, zeigen diese synthetischen Polymere in direktem Vergleich erhebliche Vorteile etwa hinsichtlich Zytotoxizät und Effizienz, was wesentlich dazu beitragen kann, aktuelle Hürden biomedizinischer Fragestellungen hinsichtlich Transport und Targeting zu überwinden. Darüber hinaus sollten zylindrische Polymerbürsten aufgrund ihrer molekularen, architekturbedingten Formanisotropie und jüngsten Ergebnissen insbesondere zur formabhängigen Endozytose sehr aussichtsreiche Kandidaten für den Einsatz zum Wirkstofftransport sein.rnrnDie vorliegende Arbeit widmete sich deshalb der Synthese und Charakterisierung von biokompatiblen zylindrischen Poly(2-oxazolin)bürsten als potentielle Nanotransporter von Wirkstoffen, Biomolekülen oder genetischem Material. Als Monomer wurde zunächst 2-Isopropyloxazolin gewählt, da das Polymer eine Phasenübergangstemperatur von 37 °C besitzt, was für Konjugatsynthesen wie auch diverse biomedizinische Applikationen interessant sein kann. Durch terminierende Methacrylamid Funktionalisierung der lebenden kationischen Oxazolinpolymerisation bzw. nachfolgende Endgruppen Transferreaktionen sind Makromonomere im Bereich 1000-5000 g/mol zugänglich. Erstmals gelang es so 2-Oxazolin basierte, hochmolekulare zylindrische Bürsten mit Konturlängen im Bereich von 250 nm mittels „Grafting Through“ Technik in freier radikalischer Polymerisation herzustellen.rnrnAusgehend von der entwickelten Syntheseroute konnten so neben Homo- und Blockcopolymerbürsten von 2-Ethyl-2-oxazolin und 2-Isopropyl-2-oxazolin auch Bürstenmoleküle aus statistischen Copolymeren von 2-Ethyl-2-oxazolin und unsubstituiertem 2-Oxazolin hergestellt werden. Während letztere die Einführung kationischer Gruppen durch selektivere Abspaltmethoden der Formylreste erlauben und so etwa DNA/RNA Komplexierungen ermöglichen können, bietet andererseits der in dieser Arbeit erstmalig demonstrierte Einsatz Azid-funktionalisierter Initiatoren zur kationischen Oxazolinpolymerisation unter Beibehaltung aller anderen sonstigen Reaktionsschritte auch die Möglichkeit der Synthese Azid-Endgruppen-funktionalisierter Makromonomere. Die „Grafting Through“ Methodik der freien radikalischen Makromonomer Polymerisation ist selbst bei diesen funktionalisierten Systemen von großem Vorteil, erlaubt sie auch hier den Zugang zu hochmolekularen Substraten mit einem Pfropfungs- bzw. Funktionalisierungsgrad von 100 %, da jede Seitenkette dieser zylindrischen Bürsten die aussenliegende, und damit sterisch leichter zugängliche funktionale Gruppe trägt. Dabei gelang es die Syntheseroute so zu gestalten, dass es möglich war alle vorgestellten Polymerbürsten mittels statischer und dynamischer Lichtstreuung hinsichtlich absoluter Molmasse und molekularer Dimension zu charakterisieren.rnIn weitereren Reaktionen konnten dann reaktive Fluoreszenzfarbstoffe mit Hilfe kupferfreier 1,3 dipolarerer Addition (kupferfreie „Click-Chemie“) an die Azid-funktionalisierten Polymerbürsten angebunden werden, so dass eine wesentliche Voraussetzung für die Detektion in in vivo und in vitro Experimenten erfüllt werden kann. Darüber hinaus gelingt die quantitative polymeranaloge Umsetzung der Azid- zu Aminogruppen durch eine polymeranalog geführte Reduktion nach Staudinger; damit können an diesen Systemen auch etablierte Konjugationstechniken an Aminogruppen durchgeführt werden. Zudem erlauben die Aminogruppen-haltigen Polymerbürsten durch Protonierung schon bei physiologischem pH die Komplexierung von DNA oder RNA. rnrnErste Lichtstreumessungen in Blutserum zeigen im Falle der kationischen Aminogruppen tragenden Polymerbürsten zwar Aggregation, was aber durch entsprechende Umsetzung nach Konjugation wahrscheinlich unterdrückt werden kann, zeigen doch die entsprechenden Precursorpolymerbürsten mit Azidgruppen in Serum keinerlei Aggregation.rnrnZellaufnahmestudien in dendritische Zellen zeigen nur im Falle einer Azid-funktionalisierten Poly(2-isopropyl-2-oxazolin)bürste eine unspezifische Aufnahme. Die hydrophileren Poly(2-oxazolin)bürsten weise keine unspezifische Aufnahme auf, was eine wichtige Anfoderung für die Verwendung als Polymercarrier in der Krebsimmuntherapie ist.rn