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Synthesis and pharmacological evaluation of pyrazine N-acylhydrazone derivatives designed as novel analgesic and anti-inflammatory drug candidates

2010; Elsevier BV; Volume: 18; Issue: 14 Linguagem: Inglês

10.1016/j.bmc.2010.06.002

1464-3391

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, Lı́dia Moreira Lima, Magna Suzana Alexandre‐Moreira,

Synthesis and Characterization of Heterocyclic Compounds

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.