| Registro completo |
| Provedor de dados: |
Anais da ABC (AABC)
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| País: |
Brazil
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| Título: |
Synthesis, X-ray diffraction study and pharmacological evaluation of 3-amino-4-methylthiophene-2-acylcarbohydrazones
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| Autores: |
HERRMANN,SONJA
SCHÜBEL,TABEA
COSTA,FANNY N.
BARBOSA,MARIA LETÍCIA C.
FERREIRA,FABIO F.
DIAS,THAYS L.M.F.
ARAÚJO,MORGANA V.
ALEXANDRE-MOREIRA,MAGNA S.
LIMA,LÍDIA M.
LAUFER,STEFAN
BARREIRO,ELIEZER J.
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| Data: |
2018-01-01
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| Ano: |
2018
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| Palavras-chave: |
N-acylhydrazone
Privileged structure
Antinociceptive
P38MAPK
X-ray
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| Resumo: |
ABSTRACT N-acylhydrazone is an interesting privileged structure that has been used in the molecular design of a myriad of bioactive compounds. In order to identify new antinociceptive drug candidates, we described herein the design, synthesis, X-ray diffraction study and the pharmacological evaluation of a series of 3-amino-4-methylthiophene-2-acylcarbohydrazone derivatives (8a-t). Compounds were prepared in good overall yields through divergent synthesis from a common key intermediate and were characterized by classical spectroscopy methods. X-ray diffraction study was employed for unequivocal determination of the imine double bond stereochemistry. 8a-t were evaluated in vivo through oral administration using the classical writhing test in mice. N-acylhydrazone derivatives 8j and 8l displayed relative potency similar to dipyrone, highlighting them as promising analgesic lead-candidates for further investigation.
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| Tipo: |
Info:eu-repo/semantics/article
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| Idioma: |
Inglês
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| Identificador: |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652018000301073
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| Editor: |
Academia Brasileira de Ciências
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| Relação: |
10.1590/0001-3765201820170796
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| Formato: |
text/html
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| Fonte: |
Anais da Academia Brasileira de Ciências v.90 n.1 suppl.2 2018
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| Direitos: |
info:eu-repo/semantics/openAccess
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