Citation: Xiang-Duan Tan, Li-Guang Mao, Wei Wu, Si-Yun Nian, Guo-Ping Wang. Synthesis and biological evaluation of substituted indazolyl amide derivatives as S-adenosyl-L-homocysteine hydrolase inhibitors[J]. Chinese Chemical Letters, ;2016, 27(6): 984-988. doi: 10.1016/j.cclet.2016.03.028 shu

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

a College of Pharmacy, Guilin Medical University, Guilin 541004, China;
b Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA;
c Zhangjiang Institute, China State Institute of Pharmaceutical Industry, Shanghai 201203, China;
d Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai 201203, China

Received Date: 25 December 2015
Revised Date: 3 March 2016

Fund Project: This research was supported by National Natural Science Foundation of China (No. 81560653) and Guangxi Natural Science Foundation of China (No. 2015GXNSFBA139124).

A series of novel amide derivatives bearing an indazole moiety were synthesized and evaluated for their in vitro S-adenosyl-L-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.
- S-Adenosylhomocysteine hydrolase,
- SAHase inhibitors,
- Amide derivatives,
- Indazole,
- Synthesis
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