Synthesis and biological evaluation of substituted indazolyl amide derivatives as S-adenosyl-L-homocysteine hydrolase inhibitors  

作　　者：Xiang-Duan Tan Li-Guang Mao Wei Wu Si-Yun Nian Guo-Ping Wang 

机构地区：[1]College of Pharmacy, Guilin Medical University [2]Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University [3]Zhangjiang Institute, China State Institute of Pharmaceutical Industry [4]Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry

出　　处：《Chinese Chemical Letters》2016年第6期984-988,共5页中国化学快报（英文版）

基　　金：supported by National Natural Science Foundation of China (No. 81560653);Guangxi Natural Science Foundation of China (No. 2015GXNSFBA139124)

摘　　要：A series of novel amide derivatives bearing an indazole moiety were synthesized and evaluated for their in vitro S-adenosylL-homocysteine hydrolase（SAHase） inhibitory activity. Among these compounds, 8b,8m, 8r and 8w showed better or similar inhibitory effects compared to the positive control aristeromycin. These results provide a novel lead for the discovery of more potent non-adenosine analogs as SAHase inhibitors.A series of novel amide derivatives bearing an indazole moiety were synthesized and evaluated for their in vitro S-adenosylL-homocysteine hydrolase（SAHase） inhibitory activity. Among these compounds, 8b,8m, 8r and 8w showed better or similar inhibitory effects compared to the positive control aristeromycin. These results provide a novel lead for the discovery of more potent non-adenosine analogs as SAHase inhibitors.

关 键 词：S-Adenosylhomocysteine hydrolase SAHase inhibitors Amide derivatives INDAZOLE SYNTHESIS 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]