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Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
Rutaecarpine derivatives synthesized via skeletal reorganization alleviate inflammation-associated oxidative damage
Nan-Ying Chen1,2, Cai-Neng Zhang1, Xiu-Yun Guo1
1Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), Guangxi Key Laboratory of Chemistry and Molecular Engineering of Medicinal Resources, School of Chemistry and Pharmaceutical Sciences, Guangxi Normal University 15 Yu Cai Road 541004 Guilin People's Republic of China chengxuepan@163.com gfysglgx@163.com.
Abstract:
In recent years, skeleton reorganization based on bioactive natural products has emerged as a novel alternative strategy to the classical approach, mainly focusing on the peripheral modification of the inherent natural skeleton. Such reorganizations not only afford structurally unique molecules but also provide unanticipated bioactivities compared with the unaltered natural precursors. Herein, by rebuilding the inherent rigid skeleton of cardioprotective rutaecarpine (RUT), thirty-three structural derivatives were designed and synthesized, with 5Ci being the most representative example, which exhibited superior protective effects against inflammation-induced ROS accumulation and cellular damage compared with the clinically used anti-inflammation drug indomethacin.
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