Design, synthesis, antinociceptive and anti-inflammatory activities of novel piroxicam analogues

Resumo

In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14a–h, planned by structural modification of piroxicam (1), a non steroidal anti-inflammatory drug. Among the synthesized analogues, compounds 14f (LASSBio-1637) and 14g (LASSBio-1639) were identified as novel antinociceptive and anti-inflammatory prototypes, active by oral administration, acting by a mechanism of action that seems to be different from that of piroxicam, since they were inactive as an inhibitor of cyclooxygenase (COX-1 and COX-2) at concentrations of 10 M.

Descrição

Palavras-chave

Piroxicam, Inflammation, Pain, Acylhydrazone, NSAID, COX

Citação

MIRANDA, Amanda Silva de; BISPO JÚNIOR, Walfrido; SILVA, Yolanda Carla Cupertino da; ALEXANDRE-MOREIRA, Magna Suzana; CASTRO, Rosane de Paula; SABINO, José Ricardo; LIÃO, Luciano Morais; LIMA, Lídia Moreira; BARREIRO, Eliezer J. Design, synthesis, antinociceptive and anti-inflammatory activities of novel piroxicam analogues. Molecules, Basel, v. 17, p. 14126-14145, 2012.