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Molecules 2017, 22(4), 512; doi:10.3390/molecules22040512

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

1
Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt
2
Department of Therapeutical Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza 12622, Egypt
3
Pharmaceutical Chemistry Department, Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
4
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)
View Full-Text   |   Download PDF [1990 KB, uploaded 24 March 2017]   |  

Abstract

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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MDPI and ACS Style

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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