Search results for "Chemical synthesi"
showing 10 items of 292 documents
Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system
2007
A series of substituted derivatives containing the 1,4-benzodioxine or pyrrole nucleus are described. All the newly synthesized compounds were examined for their in vitro and in vivo anti-inflammatory activity. Several derivatives, including (S)-2, 14 and 17, showed more anti-inflammatory activity in vivo in these assays (rat paw oedema induced by carrageenan) than the known classical anti-inflammatory agent ibuprofen, whereas other compounds like 1 were equipotent to ibuprofen. Compound 17 was the most outstanding derivative because of its remarkable in vivo anti-inflammatory activity. In this paper, we examine and discuss the structure-activity relationships and anti-inflammatory activiti…
Novel Potent Anticonvulsant Agent Containing a Tetrahydroisoquinoline Skeleton
2006
In our studies on the development of new anticonvulsants, we planned the synthesis of N-substituted 1,2,3,4-tetrahydroisoquinolines to explore the structure-activity relationships. All derivatives were evaluated against audiogenic seizures in DBA/2 mice, and the 1-(4'-bromophenyl)-6,7-dimethoxy-2-(piperidin-1-ylacetyl) derivative (26) showed the highest activity with a potency comparable to that of talampanel, the only noncompetitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonist in clinical trials as an anticonvulsant agent. Electrophysiological experiments indicated that 26 acts as noncompetitive AMPA receptor modulator.
Regioisomeric 5(3)-aminomethyl-3(5)-phenylisoxazoles: synthesis, spectroscopic discrimination, and muscarinic activity.
1995
The regioselective synthesis of isomeric 5(3)-aminomethyl-3(5)-phenyl isoxazoles using different methods is described. Spectroscopic data, especially mass spectrometric fragmentation, were used to identify and characterize the regioisomers. The muscarinic activity of these isoxazoles was assayed on isolated guinea-pig ileum and atria as well as on isolated rabbit vas deferens. Regioisomere 5(3)-Aminomethyl-3(5)-phenyl-isoxazole: Synthese, spektroskopische Unterscheidung und muskarinische Aktivitat Es werden verschiedene Verfahren zur regioselektiven Darstellung von 5(3)-Aminomethyl-3(5)-phenyl-isoxazolen beschrieben, die anhand ihrer spektroskopischen Daten, insbesondere der massenspektrosk…
Amino Acid Derivatives as Palmitoylethanolamide Prodrugs: Synthesis, In Vitro Metabolism and In Vivo Plasma Profile in Rats
2015
Palmitoylethanolamide (PEA) has antinflammatory and antinociceptive properties widely exploited in veterinary and human medicine, despite its poor pharmacokinetics. Looking for prodrugs that could progressively release PEA to maintain effective plasma concentrations, we prepared carbonates, esters and carbamates at the hydroxyl group of PEA. Chemical stability (pH 7.4) and stability in rat plasma and liver homogenate were evaluated by in vitro assays. Carbonates and carbamates resulted too labile and too resistant in plasma, respectively. Ester derivatives, prepared by conjugating PEA with various amino acids, allowed to modulate the kinetics of PEA release in plasma and stability in liver …
Phenylamides of 1-Phenyl (or Methyl)-5-benzamidopyrazole-4-carboxylic Acid as Vratizolin Analogs with Analgesic and Antiinflammatory Activities
2001
A number of phenylamides of 5-benzamidopyrazole-4-carboxylic acid were prepared in 50-80 % yields from 1-phenyl (or methyl) 6-phenylpyrazolo[3,4-d]1,3-oxazin-4(1H)-ones and aniline derivatives. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their ulcerogenic potential and acute toxicity. Some derivatives, when compared to phenylbutazone, proved more active in the tests for analgesie and antiexudative activities, but less active in the carrageenin paw oedema test. The compounds proved to posses marginal or no ulcerogenic effect, as well as low systemic toxicity.
Synthesis of Densely Packaged, Ultrasmall Pt02Clusters within a Thioether-Functionalized MOF: Catalytic Activity in Industrial Reactions at Low Tempe…
2018
The gram-scale synthesis, stabilization, and characterization of well-defined ultrasmall subnanometric catalytic clusters on solids is a challenge. The chemical synthesis and X-ray snapshots of Pt02 clusters, homogenously distributed and densely packaged within the channels of a metal-organic framework, is presented. This hybrid material catalyzes efficiently, and even more importantly from an economic and environmental viewpoint, at low temperature (25 to 140 °C), energetically costly industrial reactions in the gas phase such as HCN production, CO2 methanation, and alkene hydrogenations. These results open the way for the design of precisely defined catalytically active ultrasmall metal c…
One-step electrochemical synthesis and physico-chemical characterization of CdSe nanotubes
2013
Abstract Stoichiometric CdSe nanotubes (NTs) with a length of ∼700 nm have been successfully grown by one-step electrochemical technique into anodic alumina membranes. Cyclovoltammetric method has been performed using porous anodic alumina as template electrode and an electrochemical bath containing Cd 2+ ions and SeO 2 . The as-prepared NTs have been identified as face-centred-cubic CdSe by XRD, while micro-Raman analysis reveals the typical peaks of nanostructured CdSe. The stoichiometric deposition of CdSe NTs formation is suggested by EDX analysis, with an average atomic percentage of Cd:Se of ∼0.93. Photoelectrochemical measurements reveal that CdSe NTs are photoactive materials with d…
Determining Magnetite/Maghemite Composition and Core–Shell Nanostructure from Magnetization Curve for Iron Oxide Nanoparticles
2018
Iron oxide magnetic nanoparticles produced by chemical synthesis are usually composed of both magnetite and maghemite phases. Information about the phase composition is typically obtained using Mos...
Manganese iron oxide superparamagnetic powder by mechanochemical processing. Nanoparticles functionalization and dispersion in a nanofluid
2012
Manganese ferrite nanoparticles were synthesized using a High-Energy Ball-Milling mechanochemical method. After 1 h of milling, the process produces a material consisting of single crystalline domain nanoparticles having a diameter of about 8 nm. Chemical properties of the synthesized powders allow an easy functionalization with citric acid. Both as-obtained and functionalized samples show superparamagnetic behaviour at room temperature, and the functionalized powder is stably dispersible in aqueous media at physiological pH. The average hydrodynamic diameter is equal to similar to 60 nm. Nanoparticles obtained by the reported High-Energy Ball-Milling method can be synthesized with high yie…
Template Electrochemical Growth and Properties of Mo Oxide Nanostructures
2014
This work is aimed at studying the growing process of nanostructures electrodeposited from molybdate aqueous solutions at different pH values into pores of polycarbonate membrane templates. The challenging issue was the opportunity to investigate a rather complex deposition process in a confined ambient, where electrochemical conditions are quite different from those usually established for deposition on a flat substrate. Nanostructures were grown from a bath containing Mo7O246– (NH4)6Mo7O24·4H2O) at different concentrations (50–100 g/L), at a constant cathodic current density of 2 mA/cm2 (electrodeposition area ∼8 cm2). Nanostructured deposit was characterized by XRD, EDS, Raman, XPS, and …