Molecules 2012-01-01

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

Amanda Silva de Miranda, Walfrido Bispo Júnior, Yolanda Karla Cupertino da Silva, Magna Suzana Alexandre-Moreira, Rosane de Paula Castro, José Ricardo Sabino, Luciano Morais Lião, Lídia Moreira Lima, Eliezer J Barreiro

Index: Molecules 17(12) , 14126-45, (2012)

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Abstract

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 mM.