30492-50-3Relevant academic research and scientific papers
Antioxidant-Conjugated 1,2,4-Triazolo[4,3- a]pyrazin-3-one Derivatives: Highly Potent and Selective Human A2A Adenosine Receptor Antagonists Possessing Protective Efficacy in Neuropathic Pain
Falsini, Matteo,Catarzi, Daniela,Varano, Flavia,Ceni, Costanza,Dal Ben, Diego,Marucci, Gabriella,Buccioni, Michela,Volpini, Rosaria,Di Cesare Mannelli, Lorenzo,Lucarini, Elena,Ghelardini, Carla,Bartolucci, Gianluca,Menicatti, Marta,Colotta, Vittoria
, p. 8511 - 8531 (2019/10/16)
New 8-amino-6-aryl-1,2,4-triazolo[4,3-a]pyrazin-3-ones were designed to obtain dual antioxidant-human A2A adenosine receptor (hA2A AR) antagonists. Two sets of compounds were synthesized, the first featuring phenol rings at the 6-pos
4-PHENYL-1,3-THIAZOLES AND 4-PHENYL-1,3-OXAZOLES DERIVATIVES AS CANNABINOID RECEPTOR LIGANDS
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Page/Page column 12, (2011/04/18)
The present invention relates to new 4-phenyl-1,3-azole derivatives having the general formula (I) wherein R1, R2, R3, R4, X, A, B, and n are variable, in a racemic form, an enantiomeric form or any combinations thereof. These compounds exhibit affinity f
Synthesis and preliminary pharmacological evaluation of aryl dithiolethiones with cyclooxygenase-2-selective inhibitory activity and hydrogen sulfide-releasing properties
Zanatta, Shannon D.,Jarrott, Bevyn,Williams, Spencer J.
scheme or table, p. 946 - 957 (2011/08/05)
A series of 5-aryl-1,2-dithiolethiones and 5-aryl-1,2-dithiole-3-ones were investigated as hydrogen sulfide-releasing anti-inflammatory drugs. Generally, phenolic acetophenones were best protected by methoxymethyl groups and the dithiolethione group insta
Synthesis and evaluation of dithiolethiones as novel cyclooxygenase inhibitors
Zanatta, Shannon D.,Manallack, David T.,Jarrott, Bevyn,Williams, Spencer J.
scheme or table, p. 459 - 461 (2011/03/20)
3H-1,2-Dithiole-3-thiones substituted with a 3,5-di-tert-butyl-4-hydroxyphenyl (DTBHP) or a 3,5-di-tert-butyl-4-methoxyphenyl group at the C5 position were prepared and their ability to inhibit the cyclooxygenase isoenzymes, COX-1 and COX-2 was evaluated. Both compounds were potent inhibitors of COX-2 (relative to rofecoxib), and while the phenol was a weak inhibitor of COX-1, the methyl ether gave no measurable inhibition. Docking studies of the two compounds into the COX-1 and -2 active sites showed that the methyl ether could only fit in the COX-2 active site whereas the phenol could be docked into both COX-1 and -2. This study reports a new mode for inhibitor binding to COX-1 and -2 and a novel structural scaffold for the development of COX-2 selective inhibitors.
DITHIOLE COMPOUNDS AS COX INHIBITORS
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, (2008/12/05)
A compound of formula (I) wherein: R1 and R2 are the same or different and are independently selected from H and a shielding group; X and Y are each independently selected from N and CH; R3 is hydroxy, alkoxy, acyloxy or a
