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

Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.
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 and 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
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
Autor: Eman S. Nossier 1, Hoda H. Fahmy 2, Nagy M. Khalifa 2,3,* , Wafaa I. El-Eraky 4 and Marawan A. Baset 4
Fuente: http://mdpi.com/