具有潜在降血糖和降血脂活性的亚芳基噻唑烷二酮类化合物的合成、生物学评价及分子模拟研究
Synthesis, biological evaluation and molecular modeling studies of arylidene-thiazolidinediones with potential hypoglycemic and hypolipidemic activities.
作者信息
da Costa Leite Lúcia Fernanda C, Veras Mourão Rosa Helena, de Lima Maria do Carmo Alves, Galdino Suely Lins, Hernandes Marcelo Zaldini, de Assis Rocha Neves Francisco, Vidal Stéphanie, Barbe Jacques, da Rocha Pitta Ivan
机构信息
Departamento de Química, Universidade Católica de Pernambuco, Brazil.
出版信息
Eur J Med Chem. 2007 Oct;42(10):1263-71. doi: 10.1016/j.ejmech.2007.02.015. Epub 2007 Mar 3.
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.
合成了新型亚芳基噻唑烷二酮（ATZDs），并在四氧嘧啶诱导的高血糖小鼠模型中进行了评估。所考虑的分子靶点是核过氧化物酶体增殖物激活受体γ（PPAR-γ），其晶体结构可在蛋白质数据银行（PDB）数据库中获取，编号为2PRG。因此，在去除2PRG结构中存在的共结晶配体后，将化合物的降血糖和降血脂活性与其对接结果进行了比较。使用Autodock 3.0.5和ADT 1.1程序进行了分子建模研究。
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