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Anti-inflammatory trends of new benzimidazole derivatives.
Future Medicinal Chemistry 2016 September 22
AIM: In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A2, lipoxygenase, COXs and lipopolysaccharides-induced secretion of TNF-α 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.
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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