Farmacologia, Toxicologia i Química Terapèutica: Enviaments recents
Ara mostrant els elements 141-160 de 675
Chiral Aminoalcohol-Derived delta-Lactams Provide Easy Access to Piperidines and Acyclic Five-Carbon Building Blocks Bearing a Tertiary and a Quaternary Stereocenter.
A procedure for the synthesis of enantiopure piperidines and acyclic building blocks (5-aminopentanols, O-protected 5-hydroxypentanenitriles) containing a tertiary and a quaternary stereocenter has been developed. Starting ...
Developmental effects and genotoxicity of ten water disinfection by-products in zebrafish
Disinfection by-products are contaminants produced during drinking water disinfection. Several DBPs have been implicated in a variety of toxic effects, mainly carcinogenic and genotoxic effects. Moreover, DBPs exposure has ...
ALOX5AP overexpression in adipose tissue leads to LXA4 production and protection against diet-induced obesity and insulin resistance
Eicosanoids, such as leukotriene B4 (LTB4) and lipoxin A4 (LXA4), may play a key role during obesity. While LTB4 is involved in adipose tissue inflammation and insulin resistance, LXA4 may exert anti-inflammatory effects ...
El consumo excesivo de fructosa en el embarazo puede dañar la placenta y provocar estrés oxidativo en los fetos
La fructosa se utiliza para fabricar el sirope de maíz rico en fructosa (HFCS, en sus siglas en inglés), el cual se usa para edulcorar gran variedad de alimentos (comidas procesadas, bollería y repostería industrial, ...
Fmoc-2-Mercaptobenzothiazole (MBT), for the Introduction of the Fmoc Moiety Free of Side-Reactions
A double side-reaction, consisting in the formation of Fmoc--Ala-OH and Fmoc--Ala-AA-OH, during the preparation of Fmoc protected amino acids (Fmoc-AA-OH) with Fmoc-OSu is discussed. Furthermore, the new Fmoc-2-MBT ...
Site selectivity in Pd-catalyzed reactions of α-diazo-α-(methoxycarbonyl)acetamides: effects of catalysts and substrate substitution in the synthesis of oxindoles and ß-lactams
The Pd-catalyzed intramolecular carbene C-H insertion of α-diazo-α-(methoxycarbonyl)acetamides to prepare oxindoles as well as β-lactams was studied. In order to identify what factors influence the selectivity of the ...
CH....X (X = O, N, p) interactions in benzyl carbamate
The crystal packing and interaction energy of benzyl carbamate, C(8)H(9)NO(2), have been analysed in detail by the PIXEL method. Benzyl carbamate forms layers of hydrogen-bonded molecules, with the layers connected by ...
Pd0-Catalyzed Intramoleculara-Arylation of Sulfones: Domino Reactions in the Synthesis of Functionalized Tetrahydroisoquinolines
A new strategy for the synthesis of tetrahydroisoquinolines based on the Pd(0)-catalyzed intramolecular α-arylation of sulfones is reported. The combination of this Pd-catalyzed reaction with intermolecular Michael and ...
Facile Access to Solifenacin Impurity K: One-Step Synthesis and an HPLC-MS Method for Its Determination.
<span style="color:rgb( 34 , 34 , 34 )">Solifenacin (SFC) is a potent muscarinic antagonist that effectively reduces bladder muscle contraction, thereby alleviating symptoms such as frequency of micturition and urgency. ...
Degradation of pheromone and plant volatile components by a same Odorant-Degrading Enzyme in the cotton leafworm, Spodoptera littoralis
Background: Odorant-Degrading Enzymes (ODEs) are supposed to be involved in the signal inactivation step within the olfactory sensilla of insects by quickly removing odorant molecules from the vicinity of the olfactory ...
A fluorogenic cyclic peptide for imaging and quantification of drug-induced apoptosis
Programmed cell death or apoptosis is a central biological process that is dysregulated in many diseases, including inflammatory conditions and cancer. The detection and quantification of apoptotic cells in vivo is hampered ...
Modulating the Biological Function of Protein by Tailoring the Adsorption Orientation on Nanoparticles
Protein orientation in nanoparticle-protein conjugates plays a crucial role in binding to cell receptors and ultimately, defines their targeting efficiency. Therefore, understanding fundamental aspects of the role of protein ...
Bempedoic Acid Restores Liver H2S Production in a Female Sprague-Dawley Rat Dietary Model of Non-Alcoholic Fatty Liver
We previously demonstrated that treatment with BemA (bempedoic acid), an inhibitor of ATP citrate lyase, significantly reduces fatty liver in a model of liver steatosis (HFHFr-female Sprague-Dawley rat fed a high-fat ...
A rhein-huprine hybrid protects erythrocyte membrane integrity against Alzheimer's disease related Abeta(1-42) peptide
Alzheimer's disease remains largely unknown, and currently there is no complete cure for the disease. New synthetic approaches have been developed to create multi-target agents, such as RHE-HUP, a rhein-huprine hybrid which ...
A multicomponent reaction platform towards multimodal near-infrared BODIPY dyes for STED and fluorescence lifetime imaging
We report a platform combining multicomponent reaction synthesis and automated cell-based screening to develop biocompatible NIR-BODIPY fluorophores. From a library of over 60 fluorophores, we optimised compound NIRBD-62c ...
Moths behaving like butterflies. Evolutionary loss of long range attractant pheromones in Castniid Moths: A Paysandisia archon model
Background: In the course of evolution butterflies and moths developed two different reproductive behaviors. Whereas butterflies rely on visual stimuli for mate location, moths use the"female calling plus male seduction" ...
Heterocycle-Based Multicomponent Reactions in Drug Discovery: From Hit Finding to Rational Design
In the context of the structural complexity necessary for a molecule to selectively display a therapeutical action and the requirements for suitable pharmacokinetics, a robust synthetic approach is essential. Typically, ...
1,2-Dimethylindole-3-sulfonyl (MIS) as protecting group for the side chain of arginine
The protection of arginine (Arg) side chains is a crucial issue in peptide chemistry because of the propensity of the basic guanidinium group to produce side reactions. Currently, sulfonyl-type protecting groups, such as ...
Informe final del tutor de pràctiques externes a empresa (curs acadèmic 2017-2018)
Aquest document és l'informe del tutor d'empresa de l'any acadèmic 2017-2018 necessaria per a l'avaluació de l'assignatura optativa pràctiques en empreses del Grau de Farmàcia de la Facultat de Farmàcia i Ciències de ...
Studies on the Regioselectivity of the Cyclization of Tryptophanol-Derived Oxazolopiperidone Lactams
Cyclization of the lactam carbonyl on the indole ring in tryptophanol-derived oxazolopiperidone lactams 2 and 6, under the classical POCl3-promoted Bischler-Napieralski conditions and under neutral conditions via the ...
