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Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors.
Hussain, Saghir; Parveen, Shagufta; Qin, Xiangyu; Hao, Xin; Zhang, Shuzhen; Chen, Xin; Zhu, Changjin; Ma, Bing.
Afiliación
  • Hussain S; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
  • Parveen S; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
  • Qin X; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
  • Hao X; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
  • Zhang S; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
  • Chen X; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
  • Zhu C; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China. Electronic address: zcj@bit.edu.cn.
  • Ma B; Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
Bioorg Med Chem Lett ; 24(9): 2086-9, 2014 May 01.
Article en En | MEDLINE | ID: mdl-24726808
ABSTRACT
A novel, non-acid series of nitroquinoxalinone derivatives was synthesized and tested for their inhibitory activity against aldose reductase as targeting enzyme. All active compounds displayed an 8-nitro group, and showed significant activity in IC50 values ranging from 1.54 to 18.17 µM. Among them 6,7-dichloro-5,8-dinitro-3-phenoxyquinoxalin-2(1H)-one (7e), exhibited the strongest aldose reductase activity with an IC50 value of 1.54 µM and a good SAR (structure-activity relationship) profile.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Quinoxalinas / Aldehído Reductasa / Inhibidores Enzimáticos Límite: Humans Idioma: En Año: 2014 Tipo del documento: Article
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Quinoxalinas / Aldehído Reductasa / Inhibidores Enzimáticos Límite: Humans Idioma: En Año: 2014 Tipo del documento: Article