102254-71-7Relevant academic research and scientific papers
N-Thio- And N-selenophenacylaniidiries: Electrophilic activation as a route to some l-hetero-3-aza-4-dimethylaminobuta-l,3-dienes
Manh, Gabriel T.,Purseigle, Franck,Dubreuil, Didier,Pradere, Jean Paul,Guingant, Andre,Danion-Bougot, Renee,Danion, Daniel,Toupet, Loic
, p. 2821 - 2828 (1999)
The preparation of 2-phenyl-4-dimethylamino-l-aza-, 1-oxa-, 1-thia-, l-selena-3-azabuta-l,3-dienes as well as their 4-methyl derivatives is described following a new heteroatom interchange reaction process. Heteronucleophilic attack at one particular reactive site of bis-electrophilic amidinium salts is the key feature of the process. In addition, we also disclose that the substituted l-oxa-3-aza- and l,3-diazabuta-l,3-dienes can be obtained by a reactional transformation cascade initiated by either silver acetate addition or tosyl azide [3+2] cycloaddition onto the CS or CSe double bonds of the 1-thia- and l-selena-3-azabuta-l,3-diene analogues. The Royal Society of Chemistry 1999.
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.
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.
