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

^*Corresponding author for this work

School of Chemistry and Chemical Engineering

Beijing Institute of Technology

Research output: Contribution to journal › Article › peer-review

18 Citations (Scopus)

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.

Original language	English
Pages (from-to)	2086-2089
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2014.03.053
Publication status	Published - 1 May 2014

Keywords

Aldose reductase inhibitors
Quinoxalinone derivatives
Structure-activity relationship

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10.1016/j.bmcl.2014.03.053

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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.",

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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T1 - Novel synthesis of nitro-quinoxalinone derivatives as aldose reductase inhibitors

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

UR - https://www.scopus.com/pages/publications/84899124242

U2 - 10.1016/j.bmcl.2014.03.053

DO - 10.1016/j.bmcl.2014.03.053

M3 - Article

C2 - 24726808

AN - SCOPUS:84899124242

SN - 0960-894X

VL - 24

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

Abstract

Keywords

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