Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors

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

doi:10.1016/j.bmcl.2014.03.053

Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors

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

^*此作品的通讯作者

化学与化工学院

Beijing Institute of Technology

科研成果: 期刊稿件 › 文章 › 同行评审

17 引用（Scopus）

摘要

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.

源语言	英语
页（从-至）	2086-2089
页数	4
期刊	Bioorganic and Medicinal Chemistry Letters
卷	24
期	9
DOI	https://doi.org/10.1016/j.bmcl.2014.03.053
出版状态	已出版 - 1 5月 2014

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10.1016/j.bmcl.2014.03.053

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Hussain, S., Parveen, S., Qin, X., Hao, X., Zhang, S., Chen, X., Zhu, C., & Ma, B. (2014). Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors. Bioorganic and Medicinal Chemistry Letters, 24(9), 2086-2089. https://doi.org/10.1016/j.bmcl.2014.03.053

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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.",

keywords = "Aldose reductase inhibitors, Quinoxalinone derivatives, Structure-activity relationship",

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

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doi = "10.1016/j.bmcl.2014.03.053",

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AU - Hussain, Saghir

AU - Parveen, Shagufta

AU - Qin, Xiangyu

AU - Hao, Xin

AU - Zhang, Shuzhen

AU - Chen, Xin

AU - Zhu, Changjin

AU - Ma, Bing

PY - 2014/5/1

Y1 - 2014/5/1

N2 - 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.

AB - 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.

KW - Aldose reductase inhibitors

KW - Quinoxalinone derivatives

KW - Structure-activity relationship

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AN - SCOPUS:84899124242

SN - 0960-894X

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SP - 2086

EP - 2089

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 9

ER -

Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors

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