title: Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors.
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.
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Saghir
authors.initials: S
authors.lastname: Hussain
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Shagufta
authors.initials: S
authors.lastname: Parveen
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Xiangyu
authors.initials: X
authors.lastname: Qin
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Hao
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Shuzhen
authors.initials: S
authors.lastname: Zhang
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Chen
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China. Electronic address: zcj@bit.edu.cn.
authors.forename: Changjin
authors.initials: C
authors.lastname: Zhu
authors.affiliation: Department of Applied Chemistry, Beijing Institute of Technology, No. 5, Zhongguancun South Street, 100081 Beijing, China.
authors.forename: Bing
authors.initials: B
authors.lastname: Ma
mesh_terms: D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D062105:Molecular Docking Simulation; D009574:Nitro Compounds / Q000737:chemistry / Q000494:pharmacology; D011810:Quinoxalines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D009574:Nitro Compounds; D011810:Quinoxalines; D000449:Aldehyde Reductase
keywords: Aldose reductase inhibitors; Quinoxalinone derivatives; Structure–activity relationship