1. Structure–activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors.
- Author
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Hussain, Saghir, Parveen, Shagufta, Hao, Xin, Zhang, Shuzhen, Wang, Wei, Qin, Xiangyu, Yang, Yanchun, Chen, Xin, Zhu, Shaojuan, Zhu, Changjin, and Ma, Bing
- Subjects
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STRUCTURE-activity relationship in pharmacology , *QUINOXALINES , *ALDOSE reductase , *ENZYME inhibitors , *SUBSTITUENTS (Chemistry) , *ALDO-keto reductases , *ALCOHOL dehydrogenase - Abstract
Abstract: Novel quinoxalinone derivatives were synthesized and tested for their inhibitory activity against aldose reductase. Among them, N1-acetate derivatives had significant activity in a range of IC50 values from low micromolar to submicromolar, and compound 15a bearing a C3-phenethyl side chain was identified as the most potent inhibitor with an IC50 value of 0.143 μM. The structure–activity studies suggested that both C3-phenethyl and C6-NO2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors. [Copyright &y& Elsevier]
- Published
- 2014
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