Data/hora: 10/06/2024 07:59:11

Provedor de dados: | Anais da Academia Brasileira de Ciências
País: | Brazil
Título: | Synthesis, X-ray diffraction study and pharmacological evaluation of 3-amino-4-methylthiophene-2-acylcarbohydrazones
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.
Data: | 2018-01-01
Ano: | 2018
Palavras-chave: | N-acylhydrazone; Privileged structure; Antinociceptive; P38MAPK; X-ray.
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.
Tipo: | Info:eu-repo/semantics/article
Idioma: | Inglês
Identificador: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652018000301073
Editor: | Academia Brasileira de Ciências
Relação: | 10.1590/0001-3765201820170796
Formato: | text/html
Fonte: | Anais da Academia Brasileira de Ciências  v.90 n.1 suppl.2 2018
Fonte: | info:eu-repo/semantics/openAccess