TY - JOUR
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 - http://www.scopus.com/inward/record.url?scp=84899124242&partnerID=8YFLogxK
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 -