Synthesis, anti-inflammatory activity and molecular docking studies of 2,5-diarylfuran amino acid derivatives


Autoria(s): Stefani, Helio Alexandre; Botteselle, Giancarlo V.; Schpector, Julio Zukerman; Caracelli, Ignez; Correa, Denis da Silva; Farsky, Sandra Helena Poliselli; Machado, Isabel Daufenback; Santin, José Roberto; Hebeda, Cristina B.
Contribuinte(s)

UNIVERSIDADE DE SÃO PAULO

Data(s)

05/11/2013

05/11/2013

2012

Resumo

A series of 2,5-diaryl substituted furans functionalized with several amino acids were synthesized and evaluated as the cyclooxygenases COX-1 and COX-2 enzymes inhibitors. The proline-substituted compound inhibited PGE(2) secretion by LPS-stimulated neutrophils, suggesting selectivity for COX-2. Molecular docking studies in the binding site of COX-2 were performed. (C) 2011 Elsevier Masson SAS. All rights reserved.

FAPESP

FAPESP [07/59404-2]

CNPq [300613/2007, 306532/2009-3, 308116/2010-0]

CNPq

CAPES (Rede Nanobiotec-Brasil) [808/2009]

CAPES (Rede NanobiotecBrasil)

Identificador

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, PARIS, v. 47, n. 1, p. 52-58, JAN, 2012

0223-5234

http://www.producao.usp.br/handle/BDPI/41091

10.1016/j.ejmech.2011.10.018

http://dx.doi.org/10.1016/j.ejmech.2011.10.018

Idioma(s)

eng

Publicador

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

PARIS

Relação

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Direitos

closedAccess

Copyright ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

Palavras-Chave #2,5-DIARYLFURAN #SUZUKI-MIYAURA #AMINO ACIDS #COX-1 AND COX-2 #DOCKING #GENETIC ALGORITHM #FURAN-DERIVATIVES #AGENTS #INHIBITION #SALTS #CYCLOOXYGENASE-2 #PROTEIN #COXIBS #COX-2 #CHEMISTRY, MEDICINAL
Tipo

article

original article

publishedVersion