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Molecules 2017, 22(4), 512;

Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents

Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt
Department of Therapeutical Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza 12622, Egypt
Pharmaceutical Chemistry Department, Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
Pharmacology Department, National Research Centre, Dokki, Cairo 12622, Egypt
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 24 January 2017 / Revised: 1 March 2017 / Accepted: 2 March 2017 / Published: 24 March 2017
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [1990 KB, uploaded 24 March 2017]   |  


With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior. View Full-Text
Keywords: 1,3-diaryl pyrazole derivatives; anti-inflammatory activity; synthesis 1,3-diaryl pyrazole derivatives; anti-inflammatory activity; synthesis

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Nossier, E.S.; Fahmy, H.H.; Khalifa, N.M.; El-Eraky, W.I.; Baset, M.A. Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents. Molecules 2017, 22, 512.

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