Farmacologia, Toxicologia i Química Terapèutica: Recent submissions
Now showing items 161-180 of 675
Synthesis of cinacalcet: an enantiopure active pharmaceutical ingredient (API)
Cinacalcet hydrochloride is the only approved drug acting as calcimimetic, a new class of compds. used in the therapy of secondary hyperparathyroidism and parathyroid carcinoma. Several generic drug manufacturers and ...
Effects of MDPV on dopamine transporter regulation in male rats. Comparison with cocaine.
RATIONALE: MDPV (3,4-methylenedioxypyrovalerone) is a synthetic cathinone present in bath salts. It is a powerful psychostimulant and blocker of the dopamine transporter (DAT), like cocaine. It is known that acute exposure ...
Enantio- and Diastereoconvergent Cyclocondensation Reactions: Synthesis of Enantiopure cis-Decahydroquinolines.
Up to four stereocenters with a well-defined configuration are generated in a single synthetic step by the cyclocondensation of (R)-phenylglycinol or (1S,2R)-1-amino-2-indanol with stereoisomeric mixtures (racemates, meso ...
Synthesis of cis-hydrindan-2,4-diones bearing an all.carbon quaternary center by a Danheiser annulation
A straightforward synthetic entry to functionalized hydrindane compounds based on a rapid assembly of the core nucleus by a Danheiser cycloaddition is reported. Valuable bicyclic building blocks containing the fused five ...
Environmental Enrichment Improves Cognitive Deficits, AD Hallmarks and Epigenetic Alterations Presented in 5xFAD Mouse Model.
Cumulative evidence shows that modifications in lifestyle factors constitute an effective strategy to modulate molecular events related to neurodegenerative diseases, confirming the relevant role of epigenetics. Accordingly, ...
Multicomponent reaction access to complex quinolines via oxidation of the povarov adducts
The tetrahydroquinolines obtained through the Povarov multicomponent reaction have been oxidized to the corresponding quinoline, giving access to a single product through a two-step sequence. Several oxidizing agents were ...
Studies on the Interaction of Isocyanides with Imines: Reaction Scope and Mechanistic Variations
The interaction of imines with isocyanides has been studied. The main product results from a sequential process involving the attack of two units of isocyanide, under Lewis acid catalysis, upon the carbon-nitrogen double ...
1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies
A series of 1,2,3,4-tetrahydrobenzo[h][1,6]naphthyridines differently substituted at positions 1, 5, and 9 have been designed from the pyrano[3,2-c]quinoline derivative 1, a weak inhibitor of acetylcholinesterase (AChE) ...
Liposomal formulations for waterproofing mucosal membranes
Liposome formulations consisting of lipids contained in the stratum corneum have been recently demonstrated to</p><p>decrease the permeability of mucosae. The permeability barrier of the mucosa is dependent on the presence ...
A bicyclic α-iminophosphonate improves cognitive decline in 5xFAD murine model of neurodegeneration
I2 receptors (I2-IR) are widely distributed in the central nervous system. I2-IR ligands are associated with a neuroprotective effect but, as I2-IR structure remains unknown, the discovery of better and more selective ...
La ingesta materna de fructosa líquida acentúa la dislipemia que origina el consumo de fructosa en la descendencia de hembra adulta
El consumo de bebidas edulcoradas ricas en fructosa ha aumentado de forma considerable en las últimas décadas, de forma paralela a la mayor incidencia de enfermedades tales como la diabetes, la obesidad y las enfermedades ...
Disease-modifying treatment with I2 imidazoline receptor ligand LSL60101 in an Alzheimer's disease mouse model: A Comparative study with donepezil
Background and Purpose: The development of effective therapeutic strategies against Alzheimer's disease (AD) remains a challenge. I2 Imidazoline receptors (I2-IR) ligands have a neuroprotective role in AD. Moreover, ...
mTOR is a Key Protein Involved in the Metabolic Effects of Simple Sugars
One of the most important threats to global human health is the increasing incidences of metabolic pathologies (including obesity, type 2 diabetes and non-alcoholic fatty liver disease), which is paralleled by increasing ...
Interaction of prion protein with acetylcholinesterase: potential pathobiological implications in prion diseases
The prion protein (PrP) binds to various molecular partners, but little is known about their potential impact on the pathogenesis of prion diseases. Here, we show that PrP can interact in vitro with acetylcholinesterase ...
Peroxisome Proliferator-Activated Receptor β/δ (PPAR β/δ) as a Potential Therapeutic Target for Dyslipidemia
Dyslipidemia is a powerful predictor of cardiovascular disease in patients at high risk (Turner et al., 1998), such as type 2 diabetic patients. Lowering of LDL-C is the prime target for treatment (2002), but even with ...
Chemical Probes for Blocking of Influenza A M2 Wild-type and S31N Channels
We report on using the synthetic aminoadamantane-CH2-aryl derivatives 1-6 as sensitive probes for blocking M2 S31N and influenza A virus (IAV) M2 wild-type (WT) channels as well as virus replication in cell culture. The ...
Amelioration of BPSD-like phenotype and cognitive decline in SAMP8 mice model accompanied by molecular changes after treatment with I2-imidazoline receptor ligand MCR5
Behavioural and Psychological Symptoms of Dementia (BPSD), including fear-anxiety- and depressive-like behaviour, are present in Alzheimer's disease (AD), together with memory decline. I2-imidazoline receptors (I2-IRs) ...
Supramolecular Hydrogels Consisting of Nanofibers Increase the Bioavailability of Curcuminoids in Inflammatory Skin Diseases
The low bioavailability of curcuminoids (CCMoids) limits their use in the treatment of inflammatory skin diseases. Our work shows that this constraint can be overcome upon their incorporation into supramolecular hydrogels ...
