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Authors: Pathak, Chandramani
Singh, Rajiv Ranjan
Yadav, Saurabh
Kapoor, Neha
Raina, Varshiesh
Gupta, Sarika
Surolia, Avadhesha
Title: Evaluation of benzothiophene carboxamides as analgesics and anti-inflammatory agents
Publisher: International Union of Biochemistry and Molecular Biology
Publication Date: Mar-2014
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. © 2014 IUBMB Life, 2014.
Issue No: 3
Appears in Collections:Molecular Sciences, Publications

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