Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors

Add time:09/26/2019    Source:sciencedirect.com

Fourteen new 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5-LOX with IC50 in the range of 0.10–9.87 μM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (IC50 = 0.10–0.56 μM). More importantly, 10f and several other compounds had comparable or stronger anti-inflammatory and analgesic activities, but better gastric tolerability in vivo, as compared with darbufelone mesilate and tenidap sodium. Therefore, our findings may aid in the design of new and safe anti-inflammatory reagents for the intervention of painful inflammatory diseases, such as rheumatoid arthritis at clinic.

We also recommend Trading Suppliers and Manufacturers of 2-METHYL-5-(METHYLSULFONYL)ANILINE (cas 1671-48-3). Pls Click Website Link as below: cas 1671-48-3 suppliers

Prev:An alternative synthesis of chlorinated biphenyl methylsulfonyl metabolites
Next:Structure–activity relationship of novel series of 1,5-disubstituted tetrazoles as cyclooxygenase-2 inhibitors: Design, synthesis, bioassay screening and molecular docking studies)