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

Autor(es)

Stefani, Hello A. ^[1] ; Botteselle, Giancarlo V. ^[1] ; Zukerman-Schpector, Julio ^[2] ; Caracelli, Ignez ^[3] ; Correa, Denis da Silva ^[4] ; Farsky, Sandra H. P. ^[1] ; Machado, Isabel D. ^[1] ; Santin, Jose R. ^[1] ; Hebeda, Cristina B. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Fac Ciencias Farmaceut, Sao Paulo - Brazil

^[2] Univ Fed Sao Carlos, Dept Quim, BR-13560 Sao Carlos, SP - Brazil

^[3] Univ Fed Sao Carlos, Dept Fis, BR-13560 Sao Carlos, SP - Brazil

^[4] Univ Fed Sao Carlos, Programa Posgrad Biotecnol, BR-13560 Sao Carlos, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 47, p. 52-58, JAN 2012.
• Citações Web of Science: 10

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. (AU)

• Processo FAPESP: 07/59404-2 - Reações entre sais de potássio de organotrifluoroboratos e espécies eletrofílicas de telúrio e haletos orgânicos
• Beneficiário: Helio Alexandre Stefani
• Modalidade de apoio: Auxílio à Pesquisa - Temático