Anti-inflammatory trends of new benzimidazole derivatives

In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A , lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-α and IL-6 in mouse RAW264.7 macrophages. Synthesized compoun...

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Published inFuture medicinal chemistry Vol. 8; no. 16; pp. 1953 - 1967
Main Authors Bukhari, Syed Nasir Abbas, Lauro, Gianluigi, Jantan, Ibrahim, Fei Chee, Chin, Amjad, Muhammad Wahab, Bifulco, Giuseppe, Sher, Hassan, Abdullah, Iskandar, Rahman, Noorsaadah Abd
Format Journal Article
LanguageEnglish
Published England Future Science Ltd 01.10.2016
Subjects
anti-inflammatory
arachidonic acid
inflammation
molecular docking
prostaglandins
arachidonic acid
anti-inflammatory
prostaglandins
molecular docking
inflammation
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Summary:In present study, the anti-inflammatory activities of a new series of benzimidazole derivatives were studied, investigating their inhibition of secretory phospholipase A , lipoxygenase, COXs and lipopolysaccharide-induced secretion of TNF-α and IL-6 in mouse RAW264.7 macrophages. Synthesized compounds effectively inhibited proinflammatory enzymes and cytokines. 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 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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ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2016-0062