Literature DB >> 18072726

New celecoxib derivatives as anti-inflammatory agents.

György Szabó1, János Fischer, Agnes Kis-Varga, Klára Gyires.   

Abstract

A series of 1,5-diarylpyrazoles with a substituted benzenesulfonamide moiety was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Some compounds, for example, (+/-)-2-[4-(5- p-tolyl-3-trifluoromethyl-pyrazole-1-yl)-benzenesulfonylaminooxy]-propionic acid 16 and its disodium salt 21, had a higher in vivo anti-inflammatory activity compared to celecoxib, despite having no in vitro COX-1 or COX-2 inhibitory activity. Their gastrointestinal side effect profile is essentially more favorable than that of celecoxib.

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Year:  2007        PMID： 18072726     DOI： 10.1021/jm070821f

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  11 in total

1.  Bifunctional conjugates with potent inhibitory activity towards cyclooxygenase and histone deacetylase.

Authors:  Idris Raji; Fatima Yadudu; Emily Janeira; Shaghayegh Fathi; Lindsey Szymczak; James Richard Kornacki; Kensei Komatsu; Jian-Dong Li; Milan Mrksich; Adegboyega K Oyelere
Journal:  Bioorg Med Chem       Date:  2016-12-24       Impact factor: 3.641

2.  2-(4-Chloro-phen-yl)-5-(3,4-dimethoxy-pheneth-yl)-6,7-dihydro-pyrazolo[1,5-a]pyrazin-4(5H)-one.

Authors:  Jin-Hua Zhang; Hua Zuo; Yong-Sheng Xie; Bao-Xiang Zhao
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-06-06

3.  Crystal structure of 6-amino-4-(3-bromo-4-meth-oxy-phen-yl)-3-methyl-2,4-di-hydro-pyrano[2,3-c]pyrazole-5-carbo-nitrile dimethyl sulfoxide monosolvate.

Authors:  Sammer Yousuf; Huma Bano; Munira Taj Muhammad; Khalid Mohammed Khan
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-06-06

4.  Crystal structure of 1-(2,4-di-nitro-phen-yl)-3,5-diphenyl-1H-pyrazole.

Authors:  Shaaban K Mohamed; Joel T Mague; Mehmet Akkurt; Mustafa R Albayati; Alaa F Mohamed
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-11-14

5.  Biological Validation of Novel Polysubstituted Pyrazole Candidates with in Vitro Anticancer Activities.

Authors:  Hoda H Fahmy; Nagy M Khalifa; Magda M F Ismail; Hend M El-Sahrawy; Eman S Nossier
Journal:  Molecules       Date:  2016-02-26       Impact factor: 4.411

6.  Synthesis of benzo[d]thiazole-hydrazone analogues: molecular docking and SAR studies of potential H+/K+ ATPase inhibitors and anti-inflammatory agents.

Authors:  Shi-Meng Wang; Gao-Feng Zha; K P Rakesh; N Darshini; T Shubhavathi; H K Vivek; N Mallesha; Hua-Li Qin
Journal:  Medchemcomm       Date:  2017-04-26       Impact factor: 3.597

7.  A new synthetic approach for pyrazolo[1,5-a]pyrazine-4(5H)-one derivatives and their antiproliferative effects on lung adenocarcinoma cell line.

Authors:  Meltem Tan Uygun; Karina Amudi; İrem Doğan Turaçlı; Nurettin Menges
Journal:  Mol Divers       Date:  2021-01-02       Impact factor: 2.943

8.  4-[5-(4-Chloro-phen-yl)-3-methyl-1H-pyrazol-1-yl]benzene-sulfonamide.

Authors:  Muhammad A Farrukh; Shaaban K Mohamed; Maqsood Ahmed; Adel A Marzouk; Samir M El-Moghazy
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-01-26

9.  Synthesis, antimicrobial activity, pharmacophore modeling and molecular docking studies of new pyrazole-dimedone hybrid architectures.

Authors:  Assem Barakat; Abdullah M Al-Majid; Bander M Al-Qahtany; M Ali; Mohamed Teleb; Mohamed H Al-Agamy; Sehrish Naz; Zaheer Ul-Haq
Journal:  Chem Cent J       Date:  2018-03-14       Impact factor: 4.215

10.  Synergy of Physico-chemical and Biological Experiments for Developing a Cyclooxygenase-2 Inhibitor.

Authors:  Palwinder Singh; Jagroop Kaur; Harpreet Kaur; Anudeep Kaur; Rajbir Bhatti
Journal:  Sci Rep       Date:  2018-07-03       Impact factor: 4.379
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