Synthesis and biological evaluation of indole-3-carboxamide derivatives as antioxidant agents  

作　　者：Erfang Huang Lan Zhang Chuying Xiao Guangpeng Meng Bingqi Zhang Jianshu Hu David Chi-Cheong Wan Qingguo Meng Zhe Jin Chun Hu 

机构地区：[1]Key Laboratory of Structure-based Drug Design&Discovery,Ministry of Education,Shenyang Pharmaceutical University,Shenyang 110016,China [2]School of Biomedical Sciences,Faculty of Medicine,The Chinese University of Hong Kong,Hong Kong,China [3]Department of Pharmacy,Yantai Univeristy,Yantai 264005,China

出　　处：《Chinese Chemical Letters》2019年第12期2157-2159,共3页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(NSFC)(No.21342006);the Program for Innovative Research Team of the Ministry of Education of China (No.IRT_14R36)

摘　　要：Oxidative stress results in various pathologies and as consequence antioxidant agents have attracted uninterrupted attention.In this paper,a novel series of indole-3-carboxamide derivatives(6 a-61) were designed and synthesized based on the melatonin structure as novel antioxidants.All of them were evaluated for the antioxidant activities in vitro against human neuroblastoma SH-SY5 Y cell line using H2 O2 radical scavenging assay.The target compounds 6 a,6 f and 6 i indicated better activities than the positive control,ascorbic acid,and 6 a exhibited the best antioxidant activity.In addition,the structureactivity relationships of the target compounds were also preliminarily summarized based on the obtained experimental data.Oxidative stress results in various pathologies and as consequence antioxidant agents have attracted uninterrupted attention.In this paper,a novel series of indole-3-carboxamide derivatives（6 a-61） were designed and synthesized based on the melatonin structure as novel antioxidants.All of them were evaluated for the antioxidant activities in vitro against human neuroblastoma SH-SY5 Y cell line using H2 O2 radical scavenging assay.The target compounds 6 a,6 f and 6 i indicated better activities than the positive control,ascorbic acid,and 6 a exhibited the best antioxidant activity.In addition,the structureactivity relationships of the target compounds were also preliminarily summarized based on the obtained experimental data.

关 键 词：HETEROCYCLE MELATONIN Indole-3-carboxamide derivatives SYNTHESIS Antioxidant activity Structure-activity relationship 

分 类 号：O626.1[理学—有机化学]