Design, synthesis and preliminary pharmacological evaluation of new non-steroidal anti-inflammatory agents having a 4-(methylsulfonyl) aniline pharmacophore.

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Monther Faisel MahdiAkeel Abdul Kadhum Jassim

Abstract

A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11-14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120-300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60-240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a...Continue Reading

References

Aug 9, 1993·The American Journal of Medicine·D L DeWittW L Smith
Jan 1, 1997·Advances in Experimental Medicine and Biology·K SeibertP Isakson
Feb 15, 2001·The American Journal of Medicine·F Catella-Lawson, L J Crofford
Aug 8, 2001·Reproductive Toxicology·A Ericson, B A Källén
Aug 31, 2001·JAMA : the Journal of the American Medical Association·D MukherjeeE J Topol
Jun 28, 2002·Cleveland Clinic Journal of Medicine·Bruce N Cronstein
Nov 19, 2003·Pharmacology·Chandrashekhar S PatilShrinivas K Kulkarni
Jan 1, 2005·Prostaglandins, Leukotrienes, and Essential Fatty Acids·Regina Botting, Samir S Ayoub
Aug 17, 2005·Circulation·Domenico Praticò, Jean-Michel Dogné
Jan 9, 2007·Journal of the American College of Cardiology·Ignatius Gerardo E Zarraga, Ernst R Schwarz
Sep 11, 2007·Biochemical and Biophysical Research Communications·Hiroki FujitaMatthew D Breyer
Sep 20, 2007·Pharmacological Reviews·Bengt SamuelssonPer-Johan Jakobsson
Jul 29, 2008·Journal of Cellular and Molecular Medicine·Nina ZidarDusan Stajer
Oct 28, 2008·Journal of Lipid Research·Carol A Rouzer, Lawrence J Marnett
Mar 27, 2010·International Journal of Cell Biology·Cyril SobolewskiMarc Diederich

❮ Previous
Next ❯

Citations

Oct 17, 2014·Medicinal Research Reviews·Sharad Kumar Suthar, Manu Sharma
Jul 23, 2015·Journal of Chemotherapy·Priyanka RaniSyed Riaz Hashim
May 2, 2013·Evidence-based Complementary and Alternative Medicine : ECAM·Kou-Zhu ZhuZheng-Hong Qin
Jun 19, 2018·Scandinavian Journal of Pain·Yang YangJian-Qiang Yu

❮ Previous
Next ❯

Related Concepts

Related Feeds

Anti-inflammatory Treatments

A drug or substance that reduces inflammation (redness, swelling, and pain) in the body. Anti-inflammatory agents block certain substances in the body that cause inflammation and swelling. Discover the latest research on anti-inflammatory treatments here