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Your search keyword '"Ma, Bing"' showing total 2 results
Start Over Author "Ma, Bing" Topic aldo-keto reductase (akr) Topic aldose reductase inhibitors Publication Year Range Last 50 years
2 results on '"Ma, Bing"'

1. Structure–activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors.

Author

Hussain, Saghir, Parveen, Shagufta, Hao, Xin, Zhang, Shuzhen, Wang, Wei, Qin, Xiangyu, Yang, Yanchun, Chen, Xin, Zhu, Shaojuan, Zhu, Changjin, and Ma, Bing

Subjects
*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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2. Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors.

Author

Hussain, Saghir, Parveen, Shagufta, Qin, Xiangyu, Hao, Xin, Zhang, Shuzhen, Chen, Xin, Zhu, Changjin, and Ma, Bing

Subjects
*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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