Journal
FUTURE MEDICINAL CHEMISTRY
Volume 8, Issue 16, Pages 1953-1967Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0062
Keywords
anti-inflammatory; arachidonic acid; inflammation; molecular docking; prostaglandins
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Funding
- Universiti Kebangsaan Malaysia (UKM) by Research Incentive Fund, Arus Perdana grant [AP-2014-023]
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Aim: In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A 2, lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-alpha and IL-6 in mouse RAW264.7 macrophages. Results: Synthesized compounds effectively inhibited proinflammatory enzymes and cytokines. Conclusion: A strong inhibition of secretory phospholipases A2 was exhibited by benzimidazole derivatives with trifluoromethyl and methoxy substitutions at position 4 of attached phenyl, whereas compound 8 containing pyridine ring substituted with amino group showed very potent 5-lipoxygenase inhibition. Molecular docking experiments were carried out to elucidate the molecular basis of the observed inhibitory activities.
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