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Design, synthesis, docking and QSAR studies of novel 3,5-diaryl p | 3969
Drug Designing: Open Access

Drug Designing: Open Access
Open Access

ISSN: 2169-0138

+44 1223 790975

Design, synthesis, docking and QSAR studies of novel 3,5-diaryl pyrazole derivatives and their evaluation as antioxidants and as immunomodulators, inhibitors of TNF-, IL-2, IL-6


International Conference and Expo on Drug Discovery & Designing

August 11-13, 2015 Frankfurt, Germany

Dalia Hussein Soliman

Scientific Tracks Abstracts: Drug Des

Abstract :

Tumor necrosis factor-α (TNF-α) is one of the major pro-inflammatory cytokines which regulates further cytokine induction,
especially IL-1, IL-6, IL-2 and IL-8. The overexpression of these cytokines has been implicated in many diseases including cancer,
immune disorders as well as inflammatory diseases like septic shock, rheumatoid arthritis (RA), multiple sclerosis and Crohn’s
disease. An example of the small molecules is the pyrazole-derived scaffolds which have been identified as immunomodulators. The
pyrazole core possesses radical-scavenging ability and even its modulation in inflammatory response was related to its considerable
antioxidant activity. Moreover, it has been reported that certain antioxidants reduce LPS-induced inflammation and fever. In this work,
a new series of pyrazole–derived immune suppressants, through IL-2, IL-6 and TNF-α inhibition, has been synthesized and evaluated
for their antioxidant capacities as well. The results showed that the new compounds had good anticytokine activity comparable
to the reference Dexamethasone especially against IL-2. They also demonstrated promising antioxidant activities. Docking of the
compounds into the active site of p38MAPKinase was also studied in addition a 2D QSAR model was generated in order to correlate
the anticytokine activity with the physicochemical properties of the target compounds.

Biography :

Dalia Hussein Soliman has completed her at the age of 35 years from AL-Azhar University and Postdoctoral studies from the same University in addition to Ain-Shams
University. She is currently working as an Associate Professor of Pharmaceutical Chemistry, Pharmaceutical Chemistry Department at the Egyptian Russian University. She
has published more than 12 papers in reputed journals.

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