Synthesis of Some New Acetanilide Derivatives as COX Inhibitors and Assessment of Analgesic/ Anti-Inflammatory Activities
The purpose of the present research was to synthesize a new series of acetanilide derivatives that would have analgesic and anti-inflammatory properties in laboratory animals (rats). IR spectroscopy, 1HNMR spectroscopy and Mass spectroscopy were used to confirm the structures of freshly synthesised...
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Veröffentlicht in: | Oriental journal of chemistry 2021-12, Vol.37 (6), p.1475-1487 |
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description | The purpose of the present research was to synthesize a new series of acetanilide derivatives that would have analgesic and anti-inflammatory properties in laboratory animals (rats). IR spectroscopy, 1HNMR spectroscopy and Mass spectroscopy were used to confirm the structures of freshly synthesised compounds. The goal of the computer analysis of synthesized compounds was to see how similar they were in terms of physicochemical properties. For this, physiochemical parameters were calculated. The result suggested the reasonable physiochemical similarity with diclofenac sodium and Indomethacin. Molecular docking studies showed that the all the test compounds perfectly docked with COX-2 enzyme with all the drug-likeness characteristics. Before start of in-vivo evaluation, in vitro cyclooxygenase (COX) inhibition assays was performed with an aim to evaluate the compounds against the protein target COX-2 which would exhibit their inhibitory activity. The test compounds (C1-C6) were subjected to analgesic activity evaluation by Eddy’s hot plate method and anti-inflammatory activity evaluation by Carageenan induced edema method respectively. |
doi_str_mv | 10.13005/ojc/370629 |
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IR spectroscopy, 1HNMR spectroscopy and Mass spectroscopy were used to confirm the structures of freshly synthesised compounds. The goal of the computer analysis of synthesized compounds was to see how similar they were in terms of physicochemical properties. For this, physiochemical parameters were calculated. The result suggested the reasonable physiochemical similarity with diclofenac sodium and Indomethacin. Molecular docking studies showed that the all the test compounds perfectly docked with COX-2 enzyme with all the drug-likeness characteristics. Before start of in-vivo evaluation, in vitro cyclooxygenase (COX) inhibition assays was performed with an aim to evaluate the compounds against the protein target COX-2 which would exhibit their inhibitory activity. The test compounds (C1-C6) were subjected to analgesic activity evaluation by Eddy’s hot plate method and anti-inflammatory activity evaluation by Carageenan induced edema method respectively.</description><identifier>ISSN: 0970-020X</identifier><identifier>EISSN: 2231-5039</identifier><identifier>DOI: 10.13005/ojc/370629</identifier><language>eng</language><publisher>Bhopal: Oriental Scientific Publishing Company</publisher><subject>Acetanilide ; Anti-inflammatory agents ; Arthritis ; Benzoates ; Chemical reactions ; Disease ; Edema ; Enzymes ; Evaluation ; Inflammation ; Inflammatory response ; Infrared spectroscopy ; Laboratory animals ; Mathematical analysis ; Molecular docking ; Phenols ; Physiochemistry ; Physiology ; Potash ; Potassium ; Sodium ; Solvents ; Synthesis ; Tumor necrosis factor-TNF</subject><ispartof>Oriental journal of chemistry, 2021-12, Vol.37 (6), p.1475-1487</ispartof><rights>2021. 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The test compounds (C1-C6) were subjected to analgesic activity evaluation by Eddy’s hot plate method and anti-inflammatory activity evaluation by Carageenan induced edema method respectively.</description><subject>Acetanilide</subject><subject>Anti-inflammatory agents</subject><subject>Arthritis</subject><subject>Benzoates</subject><subject>Chemical reactions</subject><subject>Disease</subject><subject>Edema</subject><subject>Enzymes</subject><subject>Evaluation</subject><subject>Inflammation</subject><subject>Inflammatory response</subject><subject>Infrared spectroscopy</subject><subject>Laboratory animals</subject><subject>Mathematical analysis</subject><subject>Molecular docking</subject><subject>Phenols</subject><subject>Physiochemistry</subject><subject>Physiology</subject><subject>Potash</subject><subject>Potassium</subject><subject>Sodium</subject><subject>Solvents</subject><subject>Synthesis</subject><subject>Tumor necrosis factor-TNF</subject><issn>0970-020X</issn><issn>2231-5039</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>BENPR</sourceid><recordid>eNotkE1LAzEQhoMoWGpP_oGAR1k7SbpJ9rjUr0Kxhyr0tqTZrE3Zj7qTVvbfG60zhxmGh4fhJeSWwQMTAOm029upUCB5dkFGnAuWpCCySzKCTEECHDbXZIK4h1jZTEiWjsiwHtqwc-iRdhVdd42jb-6b5tYF0_ral44-ut6fTPAnh9Qgna82dNHu_NaHro-XtqQ5okNsXBt-JXlr6s9otNO4Bp8s2qo2TWMiPkRxFPngHd6Qq8rU6Cb_c0w-np_e56_JcvWymOfLxHKuQyKUM9Lamd6mplRMguClVulMamCgjVWCV1LHTgGE40ZWRsjUloKZKiuhFGNyd_Ye-u7r6DAU--7Yxx-x4BpUpgVTMlL3Z8r2HWLvquLQ-8b0Q8Gg-Iu3iPEW53jFD_NhbXk</recordid><startdate>20211230</startdate><enddate>20211230</enddate><creator>Singh, Rajib Kumar</creator><creator>Kumar, Arvind</creator><creator>Mishra, Arun K.</creator><general>Oriental Scientific Publishing Company</general><scope>AAYXX</scope><scope>CITATION</scope><scope>8FE</scope><scope>8FG</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>HCIFZ</scope><scope>KB.</scope><scope>PDBOC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope></search><sort><creationdate>20211230</creationdate><title>Synthesis of Some New Acetanilide Derivatives as COX Inhibitors and Assessment of Analgesic/ Anti-Inflammatory Activities</title><author>Singh, Rajib Kumar ; 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IR spectroscopy, 1HNMR spectroscopy and Mass spectroscopy were used to confirm the structures of freshly synthesised compounds. The goal of the computer analysis of synthesized compounds was to see how similar they were in terms of physicochemical properties. For this, physiochemical parameters were calculated. The result suggested the reasonable physiochemical similarity with diclofenac sodium and Indomethacin. Molecular docking studies showed that the all the test compounds perfectly docked with COX-2 enzyme with all the drug-likeness characteristics. Before start of in-vivo evaluation, in vitro cyclooxygenase (COX) inhibition assays was performed with an aim to evaluate the compounds against the protein target COX-2 which would exhibit their inhibitory activity. 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subjects | Acetanilide Anti-inflammatory agents Arthritis Benzoates Chemical reactions Disease Edema Enzymes Evaluation Inflammation Inflammatory response Infrared spectroscopy Laboratory animals Mathematical analysis Molecular docking Phenols Physiochemistry Physiology Potash Potassium Sodium Solvents Synthesis Tumor necrosis factor-TNF |
title | Synthesis of Some New Acetanilide Derivatives as COX Inhibitors and Assessment of Analgesic/ Anti-Inflammatory Activities |
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