1023740-23-9Relevant academic research and scientific papers
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.
, 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.
, 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
