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Pyrazolobenzotriazinone Derivatives as COX Inhibitors: Synthesis, Biological Activity, and Molecular-Modeling Studies.
MedLine Citation:
PMID:  21110338     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
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.
Authors:
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:
Type:  Journal Article    
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  343     ISSN:  1521-4184     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-11-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  631-8     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutical Chemistry and Technology, University of Palermo, Palermo, Italy.
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