Pyrazolobenzotriazinone derivatives as COX inhibitors: synthesis, biological activity, and molecular-modeling studies.

Giuseppe Tringali, D Raffa, O Migliara, B Maggio, F Plescia, S Cascioferro, Mg Cusimano, C Cannizzaro, F. Plescia

Risultato della ricerca: Contributo in rivistaArticolo in rivista

26 Citazioni (Scopus)

Abstract

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.
Lingua originaleEnglish
pagine (da-a)631-638
Numero di pagine8
RivistaArchiv der Pharmazie
Stato di pubblicazionePubblicato - 2010

Keywords

  • 4(3H)-Benzotriazinones
  • COX-2 inhibitors

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