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Molecules 2012, 17(12), 14126-14145; doi:10.3390/molecules171214126

Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues

1,2, 3,4, 3,4, 3,4, 5, 5, 6, 1,2 and 1,2,*
Received: 6 November 2012 / Revised: 19 November 2012 / Accepted: 20 November 2012 / Published: 28 November 2012
(This article belongs to the Section Medicinal Chemistry)
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In this paper we report the design, synthesis, antinociceptive and anti-inflammatory activities of a series of benzothiazine N-acylhydrazones 14ah, 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.
Keywords: piroxicam; inflammation; pain; acylhydrazone; NSAID; COX piroxicam; inflammation; pain; acylhydrazone; NSAID; COX
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


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de Miranda, A.S.; Júnior, W.B.; da Silva, Y.K.C.; Alexandre-Moreira, M.S.; Castro, R.P.; Sabino, J.R.; Lião, L.M.; Lima, L.M.; Barreiro, E.J. Design, Synthesis, Antinociceptive and Anti-Inflammatory Activities of Novel Piroxicam Analogues. Molecules 2012, 17, 14126-14145.

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