Document Detail

Pyrazolobenzotriazinone Derivatives as COX Inhibitors: Synthesis, Biological Activity, and Molecular-Modeling Studies.
MedLine Citation:
PMID:  21110338     Owner:  NLM     Status:  In-Data-Review    
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.
Demetrio Raffa; Onofrio Migliara; Benedetta Maggio; Fabiana Plescia; Stella Cascioferro; Maria Grazia Cusimano; Giuseppe Tringali; Carla Cannizzaro; Fulvio Plescia
Related Documents :
19625188 - Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as hiv-1 i...
15911248 - Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyri...
21110338 - Pyrazolobenzotriazinone derivatives as cox inhibitors: synthesis, biological activity, ...
9599228 - 32-ascomycinyloxyacetic acid derived immunosuppressants. independence of immunophilin b...
17177748 - Superficial chemical peels.
11555168 - Incorporation, distribution, and metabolism of polyunsaturated fatty acids in the pinea...
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    
Department of Pharmaceutical Chemistry and Technology, University of Palermo, Palermo, Italy.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Quantum-dot-encoded microbeads for multiplexed genetic detection of non-amplified DNA samples.
Next Document:  Synthesis and in vitro Anticancer Activities of some Selenadiazole Derivatives.