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 18.17μM. 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]