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1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.

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).

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Abdellatif KR,Elshemy HA,Azoz AA

doi

10.1016/j.bioorg.2015.09.002

subject

Has Abstract

pub_date

2015-12-01 00:00:00

pages

13-23

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(15)30017-1

journal_volume

63

pub_type

杂志文章

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