Green fluorescent protein chromophore derivatives as a new class of aldose reductase inhibitors
作者: Ryota SaitoMaiko HoshiAkihiro KatoChikako IshikawaToshiya Komatsu
作者单位: 1Department of Chemistry, Toho University, 2-2-1 Miyama, Funabashi, Chiba, 274-8510 Japan
2Research Center for Materials with Integrated Properties, Toho University, 2-2-1 Miyama, Funabashi, Chiba 274-8510, Japan
3Faculty of Pharmaceutical Science, Toho University, 2-2-1 Miyama, Funabashi, Chiba, 274-8510 Japan
4Kowa Company, Ltd., 3-4-14 Nihonbashi-honcho, Chuo-ku, Tokyo 103-8433, Japan
刊名: European Journal of Medicinal Chemistry, 2017, Vol.125 , pp.965-974
来源数据库: Elsevier Journal
DOI: 10.1016/j.ejmech.2016.10.016
关键词: Aldose reductase inhibitorDrug candidates for diabetic complicationsGFP chromophore model( Z )-4-Arylmethylene-1 H -imidazol-5(4 H )-onesDocking study
英文摘要: Abstract(#br)A number of ( Z )-4-arylmethylene-1 H -imidazol-5(4 H )-ones, which are related to the fluorescent chromophore of the Aequorea green fluorescent protein (GFP), have been synthesized and evaluated their in vitro inhibitory activity against recombinant human aldose reductase for the first time. The GFP chromophore model 1a , with a p -hydroxy group on the 4-benzylidene and a carboxymethyl group on the N1 position, exhibited strong bioactivity with an IC 50 value of 0.36 μM. This efficacy is higher than that of sorbinil, a known highly potent aldose reductase inhibitor. Compound 1h , the 2-naphtylmethylidene analogue of 1a , exhibited the best inhibitory effect among the tested copounds with an IC 50 value of 0.10 μM. Structure-activity relationship studies combined with docking...
全文获取路径: Elsevier  (合作)
影响因子:3.499 (2012)

  • chromophore 发色团
  • fluorescent 萤光的
  • aldose 醛糖
  • protein 蛋白质
  • reductase 还原酶
  • class 
  • derivatives 派生物