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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Evaluation of Some Hydrazone Derivatives as Anti-inflammatory Agents

Author(s): Zafer Asim Kaplancikli, Mehlika Dilek Altintop, Ahmet Ozdemir, Gulhan Turan-Zitouni, Shabana I. Khan and Nurhayat Tabanca

Volume 9, Issue 3, 2012

Page: [310 - 315] Pages: 6

DOI: 10.2174/157018012799129828

Price: $65

Abstract

In the present study, some hydrazone derivatives were synthesized via the reaction of 3-cyclohexylpropionic acid hydrazide with various benzaldehydes. The chemical structures of the compounds were elucidated by spectroscopic techniques such as IR, 1H-NMR and FAB-MS and elemental analyses. The compounds were evaluated for their antiinflammatory and cytotoxic activities. Anti-inflammatory activity was determined in terms of inhibition of NF-κB, ROS generation and iNOS activity. Several derivatives inhibited NF-κB and iNOS, but no effect was observed on intracellular ROS generation. Furthermore no cytoxicity was observed. Biological activity compared with the chemical structural information suggests that different functional groups on the phenyl ring influence the physicochemical properties and thus modulate biological activity.

Keywords: Hydrazone, Anti-inflammatory activity, Cytotoxicity, Antioxidant activity, Inflammation, Nonsteroidal anti-inflammatory drugs (NSAIDs), COX, Hydrazone Derivative, 1H-NMR, inflammatory activity, Chemical shifts, Proton nuclear magnetic resonance, HL-60, non-fluorescent probe


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