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

被引：13

作者：

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
]}

机构：

[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

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 47卷

基金：

巴西圣保罗研究基金会;

关键词：

2,5-Diarylfuran; Suzuki-Miyaura; Amino acids; COX-1 and COX-2; Docking; GENETIC ALGORITHM; INHIBITION; COXIBS; COX-2; SALTS;

D O I：

10.1016/j.ejmech.2011.10.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：52 / 58

页数：7

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