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Impairment of locomotor activity induced by the novelN-acylhydrazone derivatives LASSBio-785 and LASSBio-786 in mice BJMBR
Silva,G.A.P.; Kummerle,A.E.; Antunes,F.; Fraga,C.A.M.; Barreiro,E.J.; Zapata-Sudo,G.; Sudo,R.T..
The N-acylhydrazone (NAH) analogues N-methyl 2-thienylidene 3,4-benzoylhydrazine (LASSBio-785) and N-benzyl 2-thienylidene 3,4-benzoylhydrazine (LASSBio-786) were prepared from 2-thienylidene 3,4-methylenedioxybenzoylhydrazine (LASSBio-294). The ability of LASSBio-785 and LASSBio-786 to decrease central nervous system activity was investigated in male Swiss mice. LASSBio-785 or LASSBio-786 (30 mg/kg, ip) reduced locomotor activity from 209 ± 26 (control) to 140 ± 18 (P < 0.05) or 146 ± 15 crossings/min (P < 0.05), respectively. LASSBio-785 (15 or 30 mg/kg, iv) also reduced locomotor activity from 200 ± 15 to 116 ± 29 (P < 0.05) or 60 ± 16 crossings/min (P < 0.01), respectively. Likewise, LASSBio-786 (15 or 30 mg/kg, iv) reduced locomotor...
Tipo: Info:eu-repo/semantics/article Palavras-chave: N-acylhydrazone; Locomotor activity; Sedation; Hypnosis; Benzodiazepine receptor; Flumazenil.
Ano: 2013 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2013000300263
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Synthesis, X-ray diffraction study and pharmacological evaluation of 3-amino-4-methylthiophene-2-acylcarbohydrazones Anais da ABC (AABC)
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..
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....
Tipo: Info:eu-repo/semantics/article Palavras-chave: N-acylhydrazone; Privileged structure; Antinociceptive; P38MAPK; X-ray.
Ano: 2018 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652018000301073
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