Anti-inflammatory trends of new benzimidazole derivatives

• Main Authors: Bukhari, S.N.A., Lauro, G., Jantan, I., Chee, C.F., Amjad, M.W., Bifulco, G., Sher, H., Abdullah, I., Rahman, N.A.
• Format: Article
• Language: English
• Published: 2017
• Institution: Universiti Tenaga Nasional

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 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. © 2016 Future Science Ltd.