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Synthesis, characterization and preliminary pharmacological evaluation of new non-steroidal anti-inflammatory pyrazoline derivatives
Monther Faisal Mahdi (1)
, Ayad Mohammed Rasheed Raauf (2) , Noor Muneer Mohammed (3,*) (1) Department of Pharmaceutical Chemistry, College of Pharmacy, Al-Mustansiriyah University, Baghdad, 10001, Iraq
(2) Department of Pharmaceutical Chemistry, College of Pharmacy, Al-Mustansiriyah University, Baghdad, 10001, Iraq
(3) Department of Pharmaceutical Chemistry, College of Pharmacy, Al-Mustansiriyah University, Baghdad, 10001, Iraq
(*) Corresponding Author
Received: 13 Sep 2015 | Revised: 03 Oct 2015 | Accepted: 10 Oct 2015 | Published: 31 Dec 2015 | Issue Date: December 2015
Abstract
A series of six pyrazoline ring derivatives as a pharmacophore were incorporated to the naproxen; to increase its size were synthesized and preliminarly evaluated as anti-inflammatory agents with expected selectivity toward COX-2 enzyme. In vivo acute anti-inflammatory effects of the final compounds (5a-f) were evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug (naproxen) produced significant reduction of paw edema with respect to the effect of control group (propylene glycol 50%, v:v). However, compound 5d and 5e show comparable effect to naproxen at all experimental time while compounds 5a, 5b and 5c produced significantly lower inhibitory effect than naproxen at time 120-240 minutes. Furthermore, compound 5f exert significantly higher paw edema reduction than naproxen at 60-240 min. Also the antibacterial activities of the final compounds were evaluated by Well Diffusion Method. All tested compounds exert significant antibacterial activity against tested Gram positive and Gram negative bacteria in comparison to dimethyl sulfoxide as control group. In comparison the antibacterial results among the tested compound 5e may regard the best one and compound 5c the lower one.
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DOI: 10.5155/eurjchem.6.4.461-467.1321
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Department of Pharmaceutical Chemistry, College of Pharmacy, Al-Mustansiriyah University, Baghdad, 10001, Iraq
Citations
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DOI: 10.3390/molecules27207126
[2]. Ayad M. R. Raauf, Rafah F. Al-Smaism, Khalida A. Thejeel, Hala Ayad M. Rasheed
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Natural Product Research 33(9), 1277, 2019
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[3]. Maysoon Mohammed Almahdi, Ahmed Elsadig Mohammed Saeed, Nadia Hanafy Metwally
Synthesis and antimicrobial activity of some new pyrazoline derivatives bearing sulfanilamido moiety
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DOI: 10.5155/eurjchem.10.1.30-36.1791
[4]. Shahlaa Zuhair Abdul-Majeed, Monther Faisal Mahdi, Suhad Faisal Hatem Al-Mugdadi
Design, Molecular Docking Studies, Synthesis and Characterization of some New 4,5-dihydro-1H- Pyrazole-1-yl acetate Derivatives as Cyclooxygenase Inhibitors
Research Journal of Pharmacy and Technology , 3382, 2022
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Synthetic Communications 48(19), 2496, 2018
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DOI Link: https://doi.org/10.5155/eurjchem.6.4.461-467.1321
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European Journal of Chemistry 2015, 6(4), 461-467 | doi: https://doi.org/10.5155/eurjchem.6.4.461-467.1321 | Get rights and content
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