Author(s): Abdellatif KR, Elshemy HA, Azoz AA
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Abstract 2-Pyrazolins 14a-l and pyrazoles 15a-l were designed as celecoxib analogs for the evaluation of their in vitro COX-1/COX-2 inhibitory activity and the in vivo anti-inflammatory activity. Compounds 14i, 15a, 15d and 15f were the most COX-2 selective derivatives (S.I.=5.93, 6.08, 5.03 and 5.27 respectively) while the pyrazoline derivatives 14g and 14i exhibited the highest AI activity (ED50=190.5 and 160.1μmol/kg po, respectively). Copyright © 2015 Elsevier Inc. All rights reserved.
This article was published in Bioorg Chem
and referenced in Chemical Sciences Journal