Literature DB >> 23567953

Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents.

Fatma A Ragab1, Nagwa M Abdel Gawad, Hanan H Georgey, Mona F Said.   

Abstract

Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms.
Copyright © 2013 Elsevier Masson SAS. All rights reserved.

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Year:  2013        PMID: 23567953     DOI: 10.1016/j.ejmech.2013.03.005

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  7 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Design, synthesis, and discovery of 5-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones and related derivatives as novel inhibitors of mPGES-1.

Authors:  Kai Ding; Ziyuan Zhou; Shuo Zhou; Yaxia Yuan; Kyungbo Kim; Ting Zhang; Xirong Zheng; Fang Zheng; Chang-Guo Zhan
Journal:  Bioorg Med Chem Lett       Date:  2018-02-08       Impact factor: 2.823

3.  Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity.

Authors:  Ashraf S Hassan; Ahmed A Askar; Ahmed M Naglah; Abdulrahman A Almehizia; Ahmed Ragab
Journal:  Molecules       Date:  2020-06-02       Impact factor: 4.411

Review 4.  Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review.

Authors:  Chuang Zhao; K P Rakesh; L Ravidar; Wan-Yin Fang; Hua-Li Qin
Journal:  Eur J Med Chem       Date:  2018-11-22       Impact factor: 6.514

5.  Structure-guided approach on the role of substitution on amide-linked bipyrazoles and its effect on their anti-inflammatory activity.

Authors:  Souraya A Domiati; Khaled H Abd El Galil; Mohammed A S Abourehab; Tamer M Ibrahim; Hanan M Ragab
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

6.  Synthesis of New Triarylpyrazole Derivatives Possessing Terminal Sulfonamide Moiety and Their Inhibitory Effects on PGE₂ and Nitric Oxide Productions in Lipopolysaccharide-Induced RAW 264.7 Macrophages.

Authors:  Mohammed S Abdel-Maksoud; Mohammed I El-Gamal; Mahmoud M Gamal El-Din; Yunji Choi; Jungseung Choi; Ji-Sun Shin; Shin-Young Kang; Kyung Ho Yoo; Kyung-Tae Lee; Daejin Baek; Chang-Hyun Oh
Journal:  Molecules       Date:  2018-10-07       Impact factor: 4.411

7.  Design, Synthesis, Molecular Docking, and Biological Evaluation of Pyrazole Hybrid Chalcone Conjugates as Potential Anticancer Agents and Tubulin Polymerization Inhibitors.

Authors:  Md Jahangir Alam; Ozair Alam; Ahmad Perwez; Moshahid Alam Rizvi; Mohd Javed Naim; Vegi G M Naidu; Mohd Imran; Mohammed M Ghoneim; Sultan Alshehri; Faiyaz Shakeel
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-24
  7 in total

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