Literature DB >> 26398140

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

Khaled R A Abdellatif1, Heba A H Elshemy2, Amany A Azoz3.   

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.

Entities:  

Keywords:  Anti-inflammatory activity; Celecoxib analogs; Cyclooxygenase-2; Pyrazole; Pyrazoline

Mesh:

Substances:

Year:  2015        PMID: 26398140     DOI: 10.1016/j.bioorg.2015.09.002

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  2 in total

1.  Deazapurine Nucleoside Analogues for the Treatment of Trichomonas vaginalis.

Authors:  Manal J Natto; Fabian Hulpia; Eric R Kalkman; Susan Baillie; Amani Alhejeli; Yukiko Miyamoto; Lars Eckmann; Serge Van Calenbergh; Harry P de Koning
Journal:  ACS Infect Dis       Date:  2021-05-11       Impact factor: 5.578

Review 2.  Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).

Authors:  G Carullo; F Galligano; F Aiello
Journal:  Medchemcomm       Date:  2016-12-12       Impact factor: 3.597

  2 in total

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