Anti-inflammatory trends of new benzimidazole derivatives

Bukhari Syed Nasir Abbas, Gianluigi Lauro, Ibrahim Jantan, Chin Fei Chee, Muhammad Wahab Amjad, Giuseppe Bifulco, Hassan Sher, Iskandar Abdullah, Noorsaadah Abd Rahman

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1953-1967
Number of pages15
JournalFuture Medicinal Chemistry
Volume8
Issue number16
DOIs
Publication statusPublished - 1 Oct 2016

Fingerprint

Secretory Phospholipase A2
Anti-Inflammatory Agents
Arachidonate 5-Lipoxygenase
Lipoxygenase
Lipopolysaccharides
Macrophages
Cytokines
Enzymes
benzimidazole
pyridine
mouse interleukin-6

Keywords

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

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Drug Discovery

Cite this

Syed Nasir Abbas, B., Lauro, G., Jantan, I., Chee, C. F., Amjad, M. W., Bifulco, G., ... Rahman, N. A. (2016). Anti-inflammatory trends of new benzimidazole derivatives. Future Medicinal Chemistry, 8(16), 1953-1967. https://doi.org/10.4155/fmc-2016-0062

Anti-inflammatory trends of new benzimidazole derivatives. / Syed Nasir Abbas, Bukhari; Lauro, Gianluigi; Jantan, Ibrahim; Chee, Chin Fei; Amjad, Muhammad Wahab; Bifulco, Giuseppe; Sher, Hassan; Abdullah, Iskandar; Rahman, Noorsaadah Abd.

In: Future Medicinal Chemistry, Vol. 8, No. 16, 01.10.2016, p. 1953-1967.

Research output: Contribution to journalArticle

Syed Nasir Abbas, B, Lauro, G, Jantan, I, Chee, CF, Amjad, MW, Bifulco, G, Sher, H, Abdullah, I & Rahman, NA 2016, 'Anti-inflammatory trends of new benzimidazole derivatives', Future Medicinal Chemistry, vol. 8, no. 16, pp. 1953-1967. https://doi.org/10.4155/fmc-2016-0062
Syed Nasir Abbas B, Lauro G, Jantan I, Chee CF, Amjad MW, Bifulco G et al. Anti-inflammatory trends of new benzimidazole derivatives. Future Medicinal Chemistry. 2016 Oct 1;8(16):1953-1967. https://doi.org/10.4155/fmc-2016-0062
Syed Nasir Abbas, Bukhari ; Lauro, Gianluigi ; Jantan, Ibrahim ; Chee, Chin Fei ; Amjad, Muhammad Wahab ; Bifulco, Giuseppe ; Sher, Hassan ; Abdullah, Iskandar ; Rahman, Noorsaadah Abd. / Anti-inflammatory trends of new benzimidazole derivatives. In: Future Medicinal Chemistry. 2016 ; Vol. 8, No. 16. pp. 1953-1967.
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