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Evaluation of benzothiophene carboxamides as analgesics and anti-inflammatory agents

Pathak, Chandramani and Singh, Rajiv Ranjan and Yadav, Saurabh and Kapoor, Neha and Raina, Varshiesh and Gupta, Sarika and Surolia, Avadhesha (2014) Evaluation of benzothiophene carboxamides as analgesics and anti-inflammatory agents. In: IUBMB LIFE, 66 (3). pp. 201-211.

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Official URL: http://dx.doi.org/10.1002/iub.1252


Nonsteroid anti-inflammatory drugs (NSAIDs) represent standard therapy for the alleviation of pain and inflammation. At present various classes of compounds have been reported as selective inhibitors of cyclooxygenase-2 (COX-2). However, they are associated with adverse side effects. To address these issues, we report here a new class of compounds that exhibit potent analgesic and anti-inflammatory response. Substituted bromo-benzothiophene carboxamides (4-11) were examined for their analgesic and anti-inflammatory properties. Our findings demonstrate that newly synthesized bromo-benzothiophene carboxamide derivatives 4, 6, and 8 attenuate nociception and inflammation at lower concentration than classical NSAIDs, such as ibuprofen. These compounds act by selectively inhibiting COX-2 and by disrupting the prostaglandin-E2-dependent positive feedback of COX-2 regulation, which was further substantiated by reduction in the levels of cytokines, chemokines, neutrophil accumulation, synthesis of prostaglandin-E2, expression of COX-2, and neutrophil activation at lower concentration than the classic NSAID ibuprofen. Toxicological study reveals that these compounds are well tolerated and metabolized to avoid any toxicity. Thus, these molecules represent a new class of analgesic and anti-inflammatory agents. (c) 2014 IUBMB Life, 66(3):201-211, 2014

Item Type: Journal Article
Publication: IUBMB LIFE
Additional Information: Copyright for this article belongs to the WILEY-BLACKWELL, USA
Keywords: anti-nociceptive; COX-2; bromo-benzothiophene caroboxamide derivatives; hyperalgesia; anti-inflammatory
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Date Deposited: 19 May 2014 05:21
Last Modified: 19 May 2014 05:21
URI: http://eprints.iisc.ac.in/id/eprint/49082

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