Farmacologia, Toxicologia i Química Terapèutica: Recent submissions
Now showing items 361-380 of 675
Avenços cap a la síntesi de les formidolides B i C
[cat] En el present treball es descriu la millora més important realitzada en el procés de la síntesi de les formidolides B i C. Aquesta millora es basa en un canvi d'estratègia per sintetitzar el nucli macrocíclic d'aquesta ...
The addition of liguid fructose to a Western-type diet in LDL-R-/- mice induces liver inflammation and fibrogenesis markers without disrupting insulin receptor signalling after an insulin challenge
A high consumption of fat and simple sugars, especially fructose, has been related to the development of insulin resistance, but the mechanisms involved in the effects of these nutrients are not fully understood. This study ...
KHK, PNPLA3 and PPAR as Novel Targets for the Anti-Steatotic Action of Bempedoic Acid
Bempedoic acid (BemA) is an ATP-citrate lyase (ACLY) inhibitor used to treat hypercholesterolemia. We studied the anti-steatotic effect of BemA, and the mechanisms involved, in a model of fatty liver in female rats obtained ...
Comparative assessment of the sensitivity of fish early-life stage, daphnia and algae to the chronic ecotoxicity of xenobiotics - perspectives for alternatives to animal testing
No-observed-effect concentrations (NOECs) are used in environmental hazard classification and labeling of chemicals and their environmental risk assessment. They are typically obtained using standard tests such as the fish ...
Synthesis of a tetrahydroimidazo-[2',1':2,3]thiazolo[5,4-c]pyridine derivative with Met inhibitory activity
A straightforward synthesis of the Met antagonist JLK1360 involving an alkylationcyclocondensation process using aminothiazole 1 and nitrophenacyl bromide 2, reduction of the nitro group, and coupling of the resulting ...
Electrochemical analysis of gold nanoparticles multifunctionalised withCytochrome c and a zinc Porphyrin
Cytochrome c (Cyt c), known for its functional redox capabilities, plays a pivotal role in biological processes such as the electron transport chain and apoptosis. However, understanding how different conjugation strategies ...
Enantioselective total synthesis of fluvirucinin B1
A convergent synthesis of fluvirucinin B1 from acid ent-6a and nitrile ent-9, involving an organocopper coupling, a stereoselective allylation, a ring-closing metathesis reaction, and a stereoselective hydrogenation as the ...
Utilización de casos clínicos en farmacología para mejorar las habilidades y actitudes en el consejo farmacéutico del estudiante de Farmacia
El estudio de la Farmacología es esencial para formar a los futuros profesionales del medicamento en el grado de Farmacia. Sin embargo, la Farmacología es una materia muy extensa que exige un alto grado no solo de aprendizaje, ...
Structure-Activity relationship of novel second-generation synthetic cathinones: Mechanism of action, locomotion, reward, and immediate-early genes
Several new synthetic cathinones, which mimic the effect of classical psychostimulants such as cocaine or MDMA, have appeared in the global illicit drug market in the last decades. In fact, the illicit drug market is ...
PPARβ/δ: A Key Therapeutic Target in Metabolic Disorders
Research in recent years on peroxisome proliferator-activated receptor (PPAR)β/δ indicates that it plays a key role in the maintenance of energy homeostasis, both at the cellular level and within the organism as a whole. ...
Total synthesis and antiproliferative activity screening of (±)-aplicyanins A, B and E and related analogs
The first total synthesis of the indole alkaloids ()-aplicyanins A, B and E, plus seventeen analogs, all in racemic form is reported. Modifications to the parent compound included changing the number of bromine substituents ...
The Tuberculosis Drug Candidate SQ109 and Its Analogs Have Multistage Activity against Plasmodium falciparum
<p>Influenza A viruses can cause a serious future threat due to frequent mutations. Amantadine and rimantadine inhibit influenza A M2 wild-type (WT) viruses by binding and blocking M2 WT channel-mediated proton current. ...
Macroautophagic process was differentially modulated by long-term moderate exercise in rat brain and peripheral tissues
The autophagic process is a lysosomal degradation pathway, which is activated during stress conditions, such as starvation or exercise. Regular exercise has beneficial effects on human health, including neuroprotection. ...
Gemini imidazolium gels enhance the photodynamic performance of porphyrins
Photodynamic therapy (PDT) successful clinical use has led to an emerging interest in the development of improved delivery systems for photosensitizers. Amongst different formulations, gels have the advantage of being ...
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 ...
The Cream of the Crop of the Medicinal Chemistry Section of Molecules 2019
The MDPI journal Molecules is organized into 25 sections that cover many different areas of the broad field of chemistry. Among them, the Medicinal Chemistry section is one of the most classical. The overarching aim of ...
Research in natural products: Amaryllidaceae ornamental plants as sources of bioactive compounds
Podeu consultar el llibre complet a: http://hdl.handle.net/2445/120717
Neuroadaptive changes and behavioral effects after a sensitization regime of MDPV
3,4-methylenedioxypyrovalerone (MDPV) is a synthetic cathinone with cocaine-like properties. In a previous work, we exposed adolescent mice to MDPV, finding sensitization to cocaine effects, and a higher vulnerability to ...
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 ...
NMDA receptor antagonists reduce amyloid-β deposition by modulating calpain-1 signaling and autophagy, rescuing cognitive impairment in 5XFAD mice
Overstimulation of N-methyl-D-aspartate receptors (NMDARs) is the leading cause of brain excitotoxicity and often contributes to neurodegenerative diseases such as Alzheimer's Disease (AD), the most common form of dementia. ...
