| Pyrazolobenzotriazinone Derivatives as COX Inhibitors: Synthesis, Biological Activity, and Molecular-Modeling Studies. | |
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MedLine Citation:
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PMID: 21110338 Owner: NLM Status: In-Data-Review |
Abstract/OtherAbstract:
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Pyrazolylbenzotriazinones are endowed with a structural analogy with the COX-2 selective inhibitor celecoxib. Considering that our research group has long been interested in the 3-pyrazolyl-substituted benzotriazinones as anti-inflammatory agents, six new pyrazolylbenzotriazinone derivatives 16a-c and 18a-c have been prepared by reacting the opportune ethyl 5-(2-aminobenzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxylate or 5-(2-aminobenzamido)-1-(pyridin-2-yl)-1H-pyrazole-4-carboxyic acid with sodium nitrite in glacial acetic acid. The biological studies revealed a good pharmacological profile for some pyrazolylbenzotriazinones and, in the case of the ethyl 5-(4-oxo-1,2,3-benzotriazin-3(4H)-yl)-1-pyridin-2-yl-1H-pyrazole-4-carboxylate, a good COX-1/COX-2 selectivity. Molecular modeling studies confirmed the obtained biological results. |
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Authors:
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Demetrio Raffa; Onofrio Migliara; Benedetta Maggio; Fabiana Plescia; Stella Cascioferro; Maria Grazia Cusimano; Giuseppe Tringali; Carla Cannizzaro; Fulvio Plescia |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Archiv der Pharmazie Volume: 343 ISSN: 1521-4184 ISO Abbreviation: Arch. Pharm. (Weinheim) Publication Date: 2010 Nov |
Date Detail:
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Created Date: 2010-11-29 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0330167 Medline TA: Arch Pharm (Weinheim) Country: Germany |
Other Details:
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Languages: eng Pagination: 631-8 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutical Chemistry and Technology, University of Palermo, Palermo, Italy. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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