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

✍ Scribed by Yisheng Lai; Lin Ma; Wenxing Huang; Xing Yu; Yihua Zhang; Hui Ji; Jide Tian

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 424 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.056

No coin nor oath required. For personal study only.

✦ Synopsis

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 IC 50 in the range of 0.10-9.87 lM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (IC 50 = 0.10-0.56 lM). 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.

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