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| 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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| Datta,Sanchita; Roy,Syamal; Manna,Madhumita. |
| Background:Visceral leishmaniasis (VL) or Kala-Azar (KA) is one of the most deadly forms of disease among all neglected tropical diseases. There are no satisfactory drugs or vaccine candidates available for this dreaded disease. Our previous studies showed promising therapeutic and prophylactic efficacy of the live, radio-attenuated parasites through intramuscular (I.M.) and intraperitoneal (I.P.) route in BALB/c mice model.Methods:The T-cell proliferation level, the mRNA expression level of inducible nitric oxide synthase (iNOS) and tumor growth factor-beta (TGF-β) genes and finally the phosphorylation levels of phosphoinositide dependent kinase 1 (PDK1), phosphoinositide 3 kinase (PI3K) and p38 mitogen activated protein kinase (p38MAPK) molecules were... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Radio-attenuated Leishmania; Parasites; PDK1; PI3K; P38MAPK. |
| Ano: 2015 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1413-86702015000100036 |
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