1. Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors.
- Author
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Hussain, Saghir, Parveen, Shagufta, Qin, Xiangyu, Hao, Xin, Zhang, Shuzhen, Chen, Xin, Zhu, Changjin, and Ma, Bing
- Subjects
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STRUCTURE-activity relationship in pharmacology , *ALDOSE reductase , *ALDO-keto reductases , *NICOTINAMIDE adenine dinucleotide phosphate , *CHEMICAL synthesis - Abstract
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 18.17μM. 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 1.54μM and a good SAR (structure–activity relationship) profile. [Copyright &y& Elsevier]
- Published
- 2014
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