In:
Future Medicinal Chemistry, Future Science Ltd, Vol. 8, No. 16 ( 2016-10), p. 1953-1967
Abstract:
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-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.
Type of Medium:
Online Resource
ISSN:
1756-8919
,
1756-8927
DOI:
10.4155/fmc-2016-0062
Language:
English
Publisher:
Future Science Ltd
Publication Date:
2016
SSG:
15,3
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