Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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Synthesis and Evaluation of Benzimidazole Derivatives as Selective COX-2 Inhibitors

Author(s): Ankita Rathore, Mujeeb-Ur-Rahman, Anees A. Siddiqui, Abuzer Ali, Mohammad Shahar Yar.

Graphical Abstract:


Abstract:

A new series of 1-{(5-substituted-alkyl/aryl-1,3,4-oxadiazol-2-yl)methyl}-2-(piperidin-1-ylmethyl)-1Hbenzimidazoles (5a-5r) was synthesized and screened for their inhibitory activity against COX (1 and 2). In vivo antiinflammatory activity of potent compounds was done by carrageenan-induced rat paw edema model. In vitro anticancer activity of synthesized compounds was also performed at the National Cancer Institute (NCI) against NCI 60 cell lines panel. Out of the 18 compounds screened, 5h, 5i, 5j and 5l were found to be potent COX-2 inhibitors in the range of IC50 0.06-0.81 μM. In vivo anti-inflammatory screening results revealed that the compounds 5h and 5j manifested profound percent protection of 72.8 and 75.0%, respectively. Compound 5f exhibited moderate cytotoxicity with 58.79% growth inhibition against SNB-75 (CNS Cancer) cell lines and moderate activity against COX-2 (IC50 = 8.0 μM).

Keywords: Anti-inflammatory, anti-cancer, benzimidazoles, lipid peroxidation, piperidine, ulcerogenicity.

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Article Details

VOLUME: 11
ISSUE: 2
Year: 2015
Page: [188 - 199]
Pages: 12
DOI: 10.2174/1573406410666140815121613
Price: $58