54 documents found, page 1 of 6

Binding of synthetic cannabinoids to human serum albumin: site characterization...

Background: The use of new psychoactive substances (NPS) has been increasing since the beginning of the 2000s, with synthetic cannabinoids being one of the most reported groups. Consumers of these drugs typically seek their known psychoactive effects, such as relaxation and euphoria. Numerous reports of morbidity and mortality have been associated with the consumption of these substances [1,2]. Therefore, toxic...

Evaluation of P-glycoprotein activity mediated by fiscalin derivatives at the r...

Background: P-glycoprotein (P-gp) is an active efflux pump that reduces xenobiotics’ accumulation inside cells, and which activity can be modulated by inhibitors, inducers and activators [1,2]. The first ones have been used to counteract the multidrug resistance (MDR) phenomena and the inducers and activators have been proposed as a therapeutic approach in intoxication scenarios. In fact, P-gp binds several unr...

Novel Edaravone Derivatives as Neuroprotective Agents for the Treatment of ALS

Background: Amyotrophic Lateral Sclerosis (ALS) is a neurodegenerative disease (ND) with limited treatment options [1]. Although with some drawbacks, Edaravone is one of the available drugs for ALS that targets oxidative stress (OS), a key factor in the pathophysiology of this disease [1]. Objective: This work aimed to evaluate the cytotoxic effects and neuroprotective potential of a new series of Edaravone der...

Disclosing the antifungal mechanisms of the Cyclam Salt H4[H2(4-CF3PhCH2)2Cycla...

Mycoses are one of the major causes of morbidity/mortality among immunocompromised individuals. Considering the importance of these infections, the World Health Organization (WHO) defined a priority list of fungi for health in 2022 that include Candida albicans as belonging to the critical priority group and Pichia kudriavzevii (Candida krusei) to the medium priority group. The existence of few available antifu...

Unraveling fiscalin derivatives' interactions with P-glycoprotein: a computatio...

Background: P-glycoprotein (P-gp), a crucial efflux transporter located on the apical membrane of vital barrier tissues, plays a critical role in the detoxification of several endobiotics and xenobiotics [1,2]. Notably, fiscalin derivatives exhibit diverse interactions with P-gp, demonstrating inhibitory or activating effects. This interaction leads to a reduction or increase in the transported substrate levels...

Synthesis and structure elucidation of dihydro-metabolites of the synthetic cat...

Background: Synthetic cathinones are new psychoactive substances widely abused due to their psychostimulant effects. Among them, pentedrone and methylone are part of the most consumed in the USA and Europe [1]. The metabolism of synthetic cathinones is well described in literature. Methylone can undergo, for instance, N-demethylation, O-demethylation, N-oxidation, and β-keto reduction to afford the metabolites ...

Neurotoxicity Evaluation of Four Structurally Similar Synthetic Cathinones in a...

Background: Synthetic cathinones are potent central nervous system (CNS) stimulants that induce diverse neurological and psychiatric effects such as delusions, hallucinations, and agitation [1]. This fast-expanding class of new psychoactive substances (NPS) represented the majority of those seized in the European Union in 2021 [2]. Despite the growing recreational use, knowledge on their neurotoxic mechanisms, ...

Halochromic silk fabric as a reversible pH-sensor based on a novel 2-aminoimida...

Textiles are important components for the development of lightweight and flexible displays useful in smart materials. In particular, halochromic textiles are fibrous materials with a color-changing ability triggered by pH variations mainly based on pH-sensitive dye molecules. Recently, a novel class of 2-aminoimidazole azo dyes was developed with distinct substituent patterns. In this work, silk fabric was func...

Red-shifted and pH-responsive imidazole-based Azo Dyes with potent antimicrobia...

A novel route is described to obtain 2 aminoimidazole azo dyes with unique substituents pattern in the heteroaryl unit that provides halochromic properties, exhibiting vibrant colours that change from magenta to deep blue. Potent antimicrobial properties against infectious yeasts were demonstrated. No cytotoxicity was detected for concentrations lower than 16 μg·mL-1

CConjugating azoimidazoles and gold nanoparticles for a synergistic antimicrobi...