Institut de Biomedicina (IBUB): Enviaments recents
Ara mostrant els elements 241-260 de 331
A General Synthetic Route to Enantiopure 5-Substituted cis-Decahydroquinolines
A practical synthetic route to enantiopure 5-substituted cisdecahydroquinolines has been developed, the key steps being a stereoselective cyclocondensation of 2-substituted 6-oxocyclohexenepropionates 2 with (R)-phenylglycinol, ...
New Visible-Light-Sensitive Dicyanocoumarin- andCOUPY-Based Caging Groups with ImprovedPhotolytic Efficiency
Photolabile protecting groups (PPGs), also known as caging groups, are valuable tools in photopharmacology. They enable precise control over the release of bioactive compounds from the corresponding caged compounds at a ...
Enantioselective Total Synthesis of (+)-Gephyrotoxin 287C
A synthesis of (+)-gephyrotoxin 287C using, (S)-phenylglycinol-derived tricyclic lactam 7 as the starting enantiomeric scaffold is reported. From the stereochemical standpoint, the key steps are the generation of the DHQ ...
The Bace1 product sAPPβ induces ER stress and inflammation and impairs insulin signaling
Objective -secretase/-site amyloid precursor protein (APP)-cleaving enzyme 1 (BACE1) is a key enzyme involved in Alzheimer's disease that has recently been implicated in insulin-independent glucose uptake in myotubes. ...
Soluble LR11/SorLA represses thermogenesis in adipose tissue and correlates with BMI in humans
Thermogenesis in brown adipose tissue (BAT) is an important component of energy expenditure in mammals. Recent studies have confirmed its presence and metabolic role in humans. Defining the physiological regulation of BAT ...
A general methodology for the enantioselective synthesis of 1-substituted tetrahydroisoquinoline alkaloids
Starting from tricyclic lactam 2 , which is easily accessible by cyclocondensation of δ‐oxoester 1 with (R )‐phenylglycinol, a three‐step synthetic route to enantiopure 1‐substituted tetrahydroisoquinolines, including ...
Biomimetic Construction of the Hydroquinoline Ring System. Diastereodivergent Enantioselective Synthesis of 2,5-Disubstituted cis-Decahydroquinolines
The straightforward enantioselective construction of the hydroquinoline ring system from 1,5-polycarbonyl derivatives, using (R)-phenyglycinol as a chiral latent form of ammonia, is reported. The process mimics the key ...
Estratègies de modulació de l'oxidació d'àcids grassos com a tractament per combatre l'obesitat
L'estil de vida actual, amb dietes d'alt contingut calòric i falta d'exercici físic, fa que la incidència d'obesitat s'incrementi notablement. Augmentar la degradació de greixos o bé reduir la ingesta calòrica poden ser ...
Association study of 37 genes related to serotonin and dopamine neurotransmission and neurotrrhopic factors in cocaine dependence
Cocaine dependence is a neuropsychiatric disorder in which both environmental and genetic factors are involved. Several processes, that include reward and neuroadaptations, mediate the transition from use to dependence. ...
Evaluation of the interactions between human serum albumin (HSA) and warfarin or diflunisal by using molecular fluorescence using two approaches
Serum albumin is the main drug transporter of the bloodstream and contains two main binding sites: Sudlow I or acidic drug binding site, and Sudlow II or benzodiazepine binding site. Warfarin, a well-known anticoagulant ...
The Spanish Ion channel Initiative (SICI) consortium: Ten years (2008-2018) of a network of excellence on ion channel research
The Spanish Ion Channel Initiative consortium (SICI, http://sici.umh.es/default.htm) started in 2008 merging the research interests of 26 Spanish multidisciplinary groups focused on ion channel investigations from the ...
Breakthroughs in Medicinal Chemistry: New targets and mechanisms, new drugs, new hopes
The Editorial Board of the Medicinal Chemistry section of the journal Molecules publishes here its first Editorial, which has been prepared by highlighting, in sub-editorials of about one hundred words, some selected ...
The Ninth data release of the Sloan Digital Sky Survey: first spectroscopic data from the SDSS-III Baryon Oscillation Spectroscopic Survey
The Sloan Digital Sky Survey III (SDSS-III) presents the first spectroscopic data from the Baryon Oscillation Spectroscopic Survey (BOSS). This ninth data release (DR9) of the SDSS project includes 535,995 new galaxy spectra ...
An integrated pharmacokinetic and pharmacodynamic study of a new drug of abuse, methylone, a synthetic cathinone sold as 'bath salts'
Material and methods. Methylone was administered to male Sprague-Dawley rats intravenously (10 mg/kg) and orally (15 and 30 mg/kg). Plasma concentrations and metabolites were characterized by LC/MS and LC-MS/MS fragmentation ...
Multigram synthesis and in vivo efficacy studies of a novel multitarget anti-Alzheimer's compound
We describe the multigram synthesis and in vivo efficacy studies of a donepezil‒huprine hybrid that has been found to display a promising in vitro multitarget profile of interest for the treatment of Alzheimer's disease ...
Endogenous LXR signaling controls pulmonary surfactant homeostasis and prevents lung inflammation
Lung type 2 pneumocytes (T2Ps) and alveolar macrophages (AMs) play crucial roles in the synthesis, recycling and catabolism of surfactant material, a lipid/protein fluid essential for respiratory function. The liver X ...
Escape from adamantane: scaffold optimization of novel P2X7 antagonists featuring complex polycycles
The adamantane scaffold, despite being widely used in medicinal chemistry, is not devoid of problems. In recent years we have developed new polycyclic scaffolds as surrogates of the adamantane group with encouraging results ...
Iron hydride radical reductive alkylation of unactivated alkenes
Iron-catalyzed hydrogen atom transfer-mediated intermolecular C−C coupling reactions between alkenes and tosylhydrazones, followed by in situ cleavage of the tosylhydrazine intermediates using Et3N, are described. The ...
Effect of the solvent on the chromatographic selectivity in reversed-phase and HILIC
In this work, the characterization of several reversed-phase and HILIC chromatographic systems is presented by means of the Abraham's solvation parameter model, focusing on the impact of solute polarizability, dipolarity, ...
Decreased brain serotonin in rbfox1 mutant zebrafish and partial reversion of behavioural alterations by the SSRI fluoxetine
RBFOX1 functions as a master regulator of thousands of genes, exerting a pleiotropic effect on numerous neurodevelopmental and psychiatric disorders. A potential mechanism by which RBFOX1 may impact these disorders is ...
