Farmacologia, Toxicologia i Química Terapèutica: Recent submissions
Now showing items 101-120 of 675
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 ...
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 ...
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 ...
Facile synthesis of azocino[4,3-b]indoles by ring-closing metathesis
The azocino[4,3-b]indole system, tricyclic substructure of the indole alkaloids apparicine and ervaticine, is efficiently assembled by ring-closing metathesis of 2-allyl-3-(allylaminomethyl)indoles. The metathesis sites ...
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 ...
Cyclocondensation reactions of 2-acyl-3-indoleacetic acid derivatives with phenylglycinol. Enantioselective synthesis of 1-substituted tetrahydro-b-carboline alkaloids
Cyclocondensation reactions between a variety of 2‐acyl‐3‐indoleacetic acid derivatives and (R )‐phenylglycinol were studied. Successful results were obtained from N ‐alkyl keto acid derivatives. The resulting tetracyclic ...
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 ...
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 ...
Developmental exposure to MDMA (ecstasy) in zebrafish embryos reproduces the neurotoxicity adverse outcome 'lower motor activity' described in humans
The recreational use of MDMA (ecstasy) by pregnant women is associated with impaired neuromotor function in infants, but the Adverse Outcome Pathway behind this effect is not clear yet. We present for the first time the ...
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 ...
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, ...
Recent advances in lamellarin alkaloids: isolation, synthesis and activity
Lamellarins are a large family of marine alkaloids with potential anticancer activity that have been isolated from diverse marine organisms, mainly ascidians and sponges. All lamellarins feature a 3,4-diarylpyrrole system. ...
Species-specific developmental toxicity in rats and rabbits: generation of a reference compound list for development of alternative testing approaches
For regulatory information requirements, developmental toxicity testing is often conducted in two mammalian species. In order to provide a set of reference compounds that could be used to explore alternative approaches to ...
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 ...
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 ...
Developmental neurotoxicity evaluation of three Chinese herbal medicines in zebrafish larvae by means of two behavioral assays: Touch-evoked response and light/dark transition
Chinese herbal medicine (CHM) is used among pregnant women. However, the question of its safety during pregnancy remains unclear. The use of these products relies on history of use data but there are specific toxicities ...
A New Family of Subnanomolar inhibitors of Soluble Epoxide Hydrolase The FASEB journal, 13 May 2022, 36, supplement 1
The pharmacological inhibition of soluble epoxide hydrolase (sEH) has been suggested as a potential therapy for the treatment of pain and inflammatory diseases through the stabilization of epoxyeicosatrienoic acids, ...
Structure-driven discovery of α,γ-diketoacid inhibitors against UL89 Herpesvirus Terminase
Human cytomegalovirus (HCMV) is an opportunistic pathogen causing a variety of severe viral infections, including irreversible congenital disabilities. Nowadays, HCMV infection is treated by inhibiting the viral DNA ...
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 ...
