Article ; Online: Design, synthesis and molecular docking of benzophenone conjugated with oxadiazole sulphur bridge pyrazole pharmacophores as anti inflammatory and analgesic agents.
2019 Volume 92, Page(s) 103220
Abstract: The prostaglandins (PG) a group of physiologically active lipid compounds having diverse hormone like effects are important mediators of the body's response to pain and inflammation, and are formed from essential fatty acids found in cell membranes. This ...
| Abstract | The prostaglandins (PG) a group of physiologically active lipid compounds having diverse hormone like effects are important mediators of the body's response to pain and inflammation, and are formed from essential fatty acids found in cell membranes. This reaction is catalyzed by cyclooxygenase, a membrane associated enzyme occurring in two isoforms, COX-1 and COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs) act by inhibiting the activity of COX. In view of this, a series of novel benzophenones conjugated with oxadiazole sulphur bridge pyrazole moiety 8a-l were designed, synthesized, characterized and subsequently evaluated for anti-inflammatory and analgesic property. The investigation of novel analogues 8a-l for potential anti-inflammatory activity showed high levels of COX-1 and COX-2 inhibitory activity. Among the series, compound 8i with electron withdrawing fluoro group at the para position of the benzoyl ring of benzophenone was characterized by highest IC |
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| MeSH term(s) | Acetic Acid ; Analgesics/chemical synthesis ; Analgesics/chemistry ; Analgesics/pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Benzophenones/chemistry ; Benzophenones/pharmacology ; Cyclooxygenase 1/metabolism ; Cyclooxygenase 2/metabolism ; Cyclooxygenase Inhibitors/chemical synthesis ; Cyclooxygenase Inhibitors/chemistry ; Cyclooxygenase Inhibitors/pharmacology ; Dose-Response Relationship, Drug ; Drug Design ; Edema/chemically induced ; Edema/drug therapy ; Formaldehyde ; Humans ; Mice ; Molecular Docking Simulation ; Molecular Structure ; Oxadiazoles/chemistry ; Oxadiazoles/pharmacology ; Pain/chemically induced ; Pain/drug therapy ; Pain Measurement ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Rats ; Structure-Activity Relationship | |||||
| Chemical Substances | Analgesics ; Anti-Inflammatory Agents, Non-Steroidal ; Benzophenones ; Cyclooxygenase Inhibitors ; Oxadiazoles ; Pyrazoles ; Formaldehyde (1HG84L3525) ; pyrazole (3QD5KJZ7ZJ) ; benzophenone (701M4TTV9O) ; Cyclooxygenase 1 (EC 1.14.99.1) ; Cyclooxygenase 2 (EC 1.14.99.1) ; Acetic Acid (Q40Q9N063P) | |||||
| Language | English | |||||
| Publishing date | 2019-08-26 | |||||
| Publishing country | United States | |||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | |||||
| ZDB-ID | 120080-x | |||||
| ISSN | 1090-2120 ; 0045-2068 | |||||
| ISSN (online) | 1090-2120 | |||||
| ISSN | 0045-2068 | |||||
| DOI | 10.1016/j.bioorg.2019.103220 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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