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

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.

A series of novel amide derivatives containing an indazole moiety were synthesized, and compound 8w exhibited the most potent SAHase inhibitory activity with an IC50 value of 0.44 μmol/L.Figure optionsDownload as PowerPoint slide