4.5 Article

Anti-inflammatory trends of new benzimidazole derivatives

期刊

FUTURE MEDICINAL CHEMISTRY
卷 8, 期 16, 页码 1953-1967

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FUTURE SCI LTD
DOI: 10.4155/fmc-2016-0062

关键词

anti-inflammatory; arachidonic acid; inflammation; molecular docking; prostaglandins

资金

  1. 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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