Literature DB >> 34818572

Investigation of the anti-inflammatory and analgesic activities of promising pyrazole derivative.

Adnan A Bekhit1, Sherry N Nasralla2, Eman J El-Agroudy3, Nahla Hamouda4, Ahmed Abd El-Fattah5, Salma A Bekhit6, Kikuko Amagase7, Tamer M Ibrahim8.   

Abstract

The development of new COX-2 inhibitors with analgesic and anti-inflammatory efficacy as well as minimal gastrointestinal, renal and cardiovascular toxicity, is of vital importance to patients suffering from chronic course pain and inflammatory conditions. This study aims at evaluating the therapeutic activity and adverse drug reactions associated with the use of the newly synthesized pyrazole derivative, compound AD732, E-4-[3-(4-methylphenyl)-5-hydroxyliminomethyl-1H-pyrazol-1-yl]benzenesulfonamide, as compared to indomethacin and celecoxib as standard agents. Anti-inflammatory activity was assessed using carrageenan-induced rat paw edema and cotton pellet granuloma tests; formalin-induced hyperalgesia and hot plate tests were done to study analgesic activity. In vitro tests to determine COX-1/COX-2 selectivity and assessment of renal and gastric toxicity upon acute exposure to AD732 were also conducted. Compound AD732 exhibited promising results; higher anti-inflammatory and analgesic effects compared to standard agents, coupled with the absence of ulcerogenic effects and minimal detrimental effects on renal function. Additionally, compound AD732 was a less potent inhibitor of COX-2 in vitro than celecoxib, which may indicate lower potential cardiovascular toxicity. It may be concluded that compound AD732 appears to be a safer and more effective molecule with promising potential for the management of pain and inflammation.
Copyright © 2021. Published by Elsevier B.V.

Entities:  

Keywords:  Analgesic effect; Anti-inflammatory activity; COX-2 inhibitors; MD; Pyrazole derivative; docking

Mesh:

Substances:

Year:  2021        PMID: 34818572     DOI: 10.1016/j.ejps.2021.106080

Source DB:  PubMed          Journal:  Eur J Pharm Sci        ISSN: 0928-0987            Impact factor:   4.384


  4 in total

1.  Bioactivity of Novel Pyrazole-Thiazolines Scaffolds against Trypanosoma cruzi: Computational Approaches and 3D Spheroid Model on Drug Discovery for Chagas Disease.

Authors:  Leonardo da Silva Lara; Guilherme Curty Lechuga; Lorraine Martins Rocha Orlando; Byanca Silva Ferreira; Bernardo Araújo Souto; Maurício Silva Dos Santos; Mirian Claudia de Souza Pereira
Journal:  Pharmaceutics       Date:  2022-05-05       Impact factor: 6.525

2.  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

3.  New pyrazolylpyrazoline derivatives as dual acting antimalarial-antileishamanial agents: synthesis, biological evaluation and molecular modelling simulations.

Authors:  Adnan A Bekhit; Eskedar T Lodebo; Ariaya Hymete; Hanan M Ragab; Salma A Bekhit; Kikuko Amagase; Afnan Batubara; Mohammed A S Abourehab; Alaa El-Din A Bekhit; Tamer M Ibrahim
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

4.  Central Composite Design (CCD) for the Optimisation of Ethosomal Gel Formulation of Punica granatum Extract: In Vitro and In Vivo Evaluations.

Authors:  Prawez Alam; Faiyaz Shakeel; Ahmed I Foudah; Sultan Alshehri; Roshan Salfi; Mohammed H Alqarni; Tariq M Aljarba
Journal:  Gels       Date:  2022-08-17
  4 in total

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