| Autor: |
da Silva YK; LaFI-Laboratório de Farmacologia e Imunidade, Instituto de Ciências Biológicas e da Saúde, Universidade Federal de Alagoas, Maceió, AL, Brazil., Augusto CV, de Castro Barbosa ML, de Albuquerque Melo GM, de Queiroz AC, de Lima Matos Freire Dias T, Júnior WB, Barreiro EJ, Lima LM, Alexandre-Moreira MS |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2010 Jul 15; Vol. 18 (14), pp. 5007-15. Date of Electronic Publication: 2010 Jun 08. |
| DOI: |
10.1016/j.bmc.2010.06.002 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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