Farmacologia, Toxicologia i Química Terapèutica: Recent submissions
Now showing items 381-400 of 675
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, ...
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 ...
Mephedrone pharmacokinetics after intravenous and oral administration in rats: relation to pharmacodynamics
Fe d'errates disponible a: http://dx.doi.org/10.1007/s00213-013-3283-6
Overexpression in <em>Plasmodium falciparum</em> of an intrinsically disordered protein segment of <em>Pf</em>UT impairs the parasite's proteostasis and reduces its growth rate
The proteome of Plasmodium falciparum exhibits a marked propensity for aggregation. This characteristic results from the parasite’s AT-rich genome, which encodes numerous proteins with long asparagine-rich stretches and ...
A DSC study of the non-isothermal cold crystallization and relaxation effects in ubiquinone and ubiquinol
Cold crystallization effects, the kinetics-dependent crystallization behaviour of amorphous ubiquinone and ubiquinol produced in a series of quenching from-the-melt experiments, have been extensively studied through the ...
Synthesis of isoquinolin-4-ols by palladium-catalysed intramolecular nucleophilic addition of aryl iodides to aldehydes
A palladium‐catalysed intramolecular nucleophilic addition of aryl iodides to aldehydes leading to tetrahydroisoquinolin‐4‐ols is reported. A variety of products were isolated in good to excellent yields. The joint ...
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 ...
Mechanistic study on the asymmetric synthesis of the Wieland-Miescher ketone analogs
The organocatalyzed synthesis of the Wieland‐Miescher ketone (WMK) via N‐sulfonyl‐binamprolinamide catalysis was investigated using experimental and computational tools. A mechanistic proposal is presented describing the ...
The combination of mdpv and ethanol results in decreased cathinone and increased alcohol levels. Study of such pharmacological interaction.
Methylenedioxypyrovalerone (MDPV) is a new cathinone psychostimulant acting as a selective dopamine transporter blocker. Due to the concomitant consumption of ethanol (EtOH) and new psychoactive substances it is of relevance ...
Samarium(II) folding cascades involving hydrogen atom transfer for the synthesis of complex polycycles
The expedient assembly of complex, natural product-like small molecules can deliver new chemical entities with the potential to interact with biological systems and inspire the development of new drugs and probes for ...
Structure-Based Virtual Screening and in vitro and in vivo Analyses Revealed Potent Methyltransferase G9a Inhibitors as Prospective Anti-Alzheimer's Agents
G9a is a lysine methyltransferase able to di-methylate lysine 9 of histone H3, promoting the repression of genes involved in learning and memory. Novel strategies based on synthesizing epigenetic drugs could regulate gene ...
Undifferentiated and differentiated PC12 cells protected by huprines against injury induced by hydrogen peroxide
Oxidative stress is implicated in the pathogenesis of neurodegenerative disorders and hydrogen peroxide (H2O2) plays a central role in the stress. Huprines, a group of potent acetylcholinesterase inhibitors (AChEIs), have ...
Glial cell reactivity and oxidative stress prevention in Alzheimer's disease mice model by an optimized NMDA receptor antagonist
In Alzheimer's disease pathology, several neuronal processes are dysregulated by excitotoxicity including neuroinflammation and oxidative stress (OS). New therapeutic agents capable of modulating such processes are needed ...
Antifungal compounds from plants
Podeu consultar el llibre complet a: http://hdl.handle.net/2445/46988
Benzofuranyl-2-imidazoles as imidazoline I2 receptor ligands for Alzheimer's disease
Recent findings unveil the pharmacological modulation of imidazoline I2 receptors (I2-IR) as a novel strategy to face unmet medical neurodegenerative diseases. In this work, we report the chemical characterization, ...
Enantioselective synthesis of lepadins A D from a phenylglycinol-derived hydroquinolone lactam
The marine alkaloids (-)-lepadins A-C and (+)-lepadin D, belonging to two diastereoisomeric series, were synthesized from an (R)-phenylglycinol-derived tricyclic lactam via a common cis-decahydroquinoline intermediate. ...
Palmitic and oleic acid: The Yin and Yang of fatty acids in type 2 diabetes mellitus
Increased plasma non-esterified fatty acids (NEFAs) link obesity with insulin resistance and type 2 diabetes mellitus (T2DM). However, in contrast to the saturated FA (SFA) palmitic acid, the monounsaturated FA (MUFA) oleic ...
Effects of High-Fat Diet and Maternal Binge-Like Alcohol Consumption and Their Influence on Cocaine Response in Female Mice Offspring
Backgroud: Prenatal alcohol exposure is a leading cause of neurobehavioral and neurocognitive deficits collectively known as fetal alcohol spectrum disorders (FASD), including eating disorders and increased risk for substance ...
