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

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.

SUBMITTER: de Miranda AS

PROVIDER: S-EPMC6268254 | biostudies-literature | 2012 Nov

REPOSITORIES: biostudies-literature

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

de Miranda Amanda Silva AS Bispo Júnior Walfrido W da Silva Yolanda Karla Cupertino YK Alexandre-Moreira Magna Suzana MS Castro Rosane de Paula Rde P Sabino José Ricardo JR Lião Luciano Morais LM Lima Lídia Moreira LM Barreiro Eliezer J EJ

Molecules (Basel, Switzerland) 20121128 12

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 tha ...[more]

PMID: 23192189

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