title: Design and synthesis of amide derivatives as S-adenosyl-L-homocysteine hydrolase inhibitors.
abstract: In this study, a series of amide derivatives were synthesized and evaluated for their S-adenosyl-L-homocysteine 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 (IC50<10.0 µM). The 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.
authors.affiliation: Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry.
authors.forename: Xiangduan
authors.initials: X
authors.lastname: Tan
authors.forename: Panfeng
authors.initials: P
authors.lastname: Wang
authors.forename: Siyun
authors.initials: S
authors.lastname: Nian
authors.forename: Guoping
authors.initials: G
authors.lastname: Wang
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives / Q000494:pharmacology; D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D006710:Homocysteine / Q000037:antagonists & inhibitors*; D006867:Hydrolases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D006710:Homocysteine; C030034:aristeromycin; D006867:Hydrolases; D000241:Adenosine