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Synthesis and biological evaluation of indole-3-carboxamide derivatives as antioxidant agents
Authors:Erfang Huang  Lan Zhang  Chuying Xiao  Guangpeng Meng  Bingqi Zhang  Jianshu Hu  David Chi-Cheong Wan  Qingguo Meng  Zhe Jin  Chun Hu
Affiliation:Key Laboratory of Structure-based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China; School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, China; Department of Pharmacy, Yantai Univeristy, Yantai 264005, China
Abstract: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 (6a-6l) 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-SY5Y cell line using H2O2 radical scavenging assay. The target compounds 6a, 6f and 6i indicated better activities than the positive control, ascorbic acid, and 6a exhibited the best antioxidant activity. In addition, the structureactivity relationships of the target compounds were also preliminarily summarized based on the obtained experimental data.
Keywords:Heterocycle  Melatonin  Indole-3-carboxamide derivatives  Synthesis  Antioxidant activity  Structure-activity relationship  
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