期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 6, 页码 2345-2352出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.02.012
关键词
Cyclooxygenase enzymes; Isoxazolo[4,5-d]pyridazin-4(5H)-one; N-Acylhydrazone; Docking
资金
- Hacettepe University [0501301001]
- Natural Sciences and Engineering Council (NSERC) of Canada
In this study, new isoxazolo[4,5-d]pyridazin-4(5H)-one derivatives having an N-acylhydrazone moiety were synthesized. The compounds were tested for their COX inhibitory activities using NS-398 and indomethacine as reference compounds. Although the compounds had an inhibitory profile against both COX-1 and COX-2, most were found to be more selective against COX-2 by a small percentage of inhibition, at the concentration of 50 mu M. Docking studies were clone to understand the interactions of the tested compounds with the active site of COX-2. It was observed that the compounds fit into, and interacted with, the hydrophobic parts which are common in the active pocket of COX-1 and COX-2 enzymes but could not fit to the area which is specific for COX-2 enzyme.
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