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A Single Amino Acid Difference between Cyclooxygenase-1 (COX-1) and -2(COX-2) Reverses the Selectivity of COX-2 Specific Inhibitors

โœ Scribed by McDonald, J. J.


Book ID
115530399
Publisher
The American Society for Biochemistry and Molecular Biology
Year
1996
Tongue
English
Weight
158 KB
Volume
271
Category
Article
ISSN
0021-9258

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A series of potent and highly selective cyclooxygenase-2 inhibitors have been prepared by replacing the benzoyl group of indomethacin with a 4-bromobenzyl group, and by extending the acetic acid side chain. These compounds show anti-inflammatory activity in rats with no evidence of GI toxicity, even