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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Abstract
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 |
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Publication: | IUBMB LIFE |
Publisher: | WILEY-BLACKWELL |
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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