67229-59-8Relevant academic research and scientific papers
Heteroarylnitrones as drugs for neurodegenerative diseases: Synthesis, neuroprotective properties, and free radical scavenger properties
Porcal, Williams,Hernández, Paola,González, Mercedes,Ferreira, Ana,Olea-Azar, Claudio,Cerecetto, Hugo,Castro, Ana
body text, p. 6150 - 6159 (2009/10/23)
New 1,2,4-thiadiazolylnitrones and furoxanylnitrones were developed and evaluated as neuroprotective agents on a human neuroblastoma (SH-SY5Y) cells model. They inhibited at low micromolar concentrations the oxidative damage and the death induced by exposure to hydrogen peroxide. These heteroarylnitrones showed excellent peroxyl free radical absorbance capacities, analyzed by oxygen radical absorbance capacity (ORAC) assay with fluorescein as the fluorescent probe, ranging from 1.5- to 16.5-fold the value of the reference nitrone, α-phenyl-N-tert-butylnitrone (PBN). The electron spin resonance spectroscopy (ESR) demonstrated the ability of these derivatives to directly trap and stabilize oxygen, carbon, and sulfur-centered free radicals. These results demonstrated the potential use of these heteroarylnitrones as neuroprotective agents in preventing the death of cells exposed to enhanced oxidative stress and damage.
Non-ATP competitive glycogen synthase kinase 3β (GSK-3β) inhibitors: Study of structural requirements for thiadiazolidinone derivatives
Castro, Ana,Encinas, Arantxa,Gil, Carmen,Braese, Stefan,Porcal, Williams,Perez, Concepcion,Moreno, Francisco J.,Martinez, Ana
, p. 495 - 510 (2008/04/05)
The 2,4-disubstituted thiadiazolidinones (TDZD) were described as the first non-ATP competitive GSK-3β inhibitors. New modifications in this heterocyclic ring are here reported to study the influence on the biological activity. The basic skeleton of 1,2,4-thiadiazole and also one of the carbonyl groups are kept, while different modifications are introduced in positions 3 and 5, respectively. The GSK-3β activity of the new thiadiazole derivatives here synthesized showed IC50 values for some of the compounds in the micromolar range. Additionally, ATP competition studies have been carried out, showing that as well as the first generation of TDZD, these new compounds act in a non-competitive manner. With this study, additional requirements for the biological activity of the TDZD family have been delineated.
THIA-1 AZA-3 BUTADIENES SUBSTITUES: ACTION DU CETENE ET DERIVES
Gokou, Celestin Tea,Chehna, Moustafa,Pradere, Jean-Paul,Duguay, Guy,Toupet, Loic
, p. 327 - 340 (2007/10/02)
Novel, diversely substituted 1-thia 3-aza butadienes have been prepared and reacted with ketene or its derivatives.Via a general (4+2) cycloaddition reaction, they afford functionalised 6H-1,3-thiazine 6-ones, the electrophilic properties of which are described.This cycloaddition gives rise to other reaction products resulting from the addition of two or three molecules of ketene according to the nature of the substituents.
The Preparation and Rearrangements of 5-acyl-2-phenyl-4-substituted 6H-1,3-Thiazines. X-Ray Molecular Structure of 3-Acetyl-2-ethoxycarbonyl-4-(3-oxobutylthio)-5-phenylpyrrole
Gokou, Celestin Tea,Pradere, Jean-Paul,Quiniou, Herve,Toupet, Loic
, p. 1875 - 1878 (2007/10/02)
5-Acyl-2-phenyl-4-substituted 6H-1,3-thiazines are prepared by the reaction of N',N'-substituted N2-thiobenzoylformamidines with methyl vinyl ketone or acrylaldehyde.Rearrangement catalysed by base and subsequent condensation with the acrylic reagent gives substituted pyrrolyl sulphides or substituted 2,6-dihydrothiopyranopyrrole.
New Synthesis of 1,2,4-Thiadiazoles
Lin, Yang-i,Lang, S. A.,Petty, Sharon R.
, p. 3750 - 3753 (2007/10/02)
A new synthesis of 1,2,4-thiadiazoles has been developed.N'-(Thioaroyl)- (and N'-arylthiocarbamoyl-) N,N-dimethylamidines, which were prepared in excellent yields by reactions of thioamides (and thioureas) with N,N-dimethylalkanamide dimethyl acetals, rea
