Design and Synthesis of Amide Derivatives as S-Adenosyl-L-Homocysteine Hydrolase Inhibitors

Xiangduan Tan, Panfeng Wang, Siyun Nian, Guoping Wang
2014 Chemical and pharmaceutical bulletin  
In this study, a series of amide derivatives were synthesized and evaluated for their S-adenosyl-Lhomocysteine hydrolase (SAHase) inhibitory activities. The results demonstrated that most of compounds displayed potent SAHase inhibitory activities. Interestingly, compounds 11 and 14 exhibited more potent inhibitory effects than the aristeromycin, one of the most potent SAHase inhibitors known so far. Compounds 12, 13, 15 and 17 exhibited a moderate effect (IC 50 <10.0 µM) . The
more » ... e structure-activity relationship found that compounds with substituted indazole-5-yl group at Ar position and ethylamino group at the side chain showed better SAHase inhibitory activities.
doi:10.1248/cpb.c13-00623 pmid:24162783 fatcat:2pquhxfsh5fexlgtf3x4o7qeka