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Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates
Yolanda Karla Cupertino da Silva ,
Cristina Villarinho Augusto ,
Maria Letícia de Castro Barbosa ,
Gabriela Muniz de Albuquerque Melo ,
Aline Cavalcanti de Queiroz ,
Thays de Lima Matos Freire Dias ,
Walfrido Bispo Júnior ,
Eliezer J. Barreiro ,
Lídia Moreira Lima ,
Magna Suzana Alexandre-Moreira
July 2010
July 2010
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Abstract
In this paper, we report the synthesis and pharmacological evaluation of pyrazine
N-acylhydrazone (NAH) derivatives (2a-s) designed as novel analgesic and anti-inflammatory
drug candidates. This series was planned by molecular simplification of prototype
1 (LASSBio-1018), previously described as a non-selective cyclooxygenase inhibitor.
Derivatives 2a-s were evaluated in several animal models of pain and inflammation,
standing-out compound 2o (2-N'-[(E)-(3,4,5-trimethoxyphenyl) methylidene]-2-pyrazinecarbohydrazide;
LASSBio-1181), that was also active in a murine model of chronic inflammation (i.e.,
adjuvant-induced arthritis test in rats) and can be considered a new analgesic and
anti-inflammatory lead for drug development.