Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities

被引:55
作者
da Costa Leite, Lucia Fernanda C.
Veras Mourao, Rosa Helena
Alves de Lima, Maria do Carmo
Galdino, Suely Lins
Hernandes, Marcelo Zaldini
Rocha Neves, Francisco de Assis
Vidal, Stephanie
Barbe, Jacques
Pitta, Ivan da Rocha [1 ]
机构
[1] Univ Fed Pernambuco, Dept Antibioticos, BR-50670901 Recife, PE, Brazil
[2] Univ Catolica Pernambuco, Dept Quim, BR-50050900 Recife, PE, Brazil
[3] Univ Brasilia, BR-70910900 Brasilia, DF, Brazil
[4] Univ Mediterranee, Fac Pharm, GERCTOP, CNRS,UMR 6178, F-13385 Marseille 5, France
关键词
arylidene-thiazolidinediones; hypoglycemic; hypolipidemic; molecular modeling; docking;
D O I
10.1016/j.ejmech.2007.02.015
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
New arylidene-thiazolidinediones (ATZDs) were synthesized and evaluated in the alloxan-induced hyperglycemia mice model. The molecular target taken into consideration is the nuclear PPAR-gamma whose crystallographic structure is available on the PDB database as 2PRG. Thus the hypoglycemic and hypolipidemic activities of compounds were compared with the result of their docking after removal of the co-crystallized ligand present in the 2PRG structure. Molecular modeling studies were carried out using the Autodock 3.0.5 and ADT 1.1 programs. (c) 2007 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:1263 / 1271
页数:9
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