title: Development of potent and selective human A3 adenosine receptor agonists.
abstract: On the basis of bioisosteric rationale, structure-activity relationship of Cl-IB-MECA, which showed high binding affinity at the human A3 adenosine receptor, was studied. From this study, 2-chloro-4'-thioadenosine-5'-methyluronamide was discovered as the most potent and selective agonist at the human A3 adenosine receptor.
authors.affiliation: Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
authors.forename: Lak Shin
authors.initials: LS
authors.lastname: Jeong
authors.forename: Hyuk Woo
authors.initials: HW
authors.lastname: Lee
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Jacobson
authors.forename: Sang Kook
authors.initials: SK
authors.lastname: Lee
authors.forename: Moon Woo
authors.initials: MW
authors.lastname: Chun
mesh_terms: D000241:Adenosine / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism; D058909:Adenosine A3 Receptor Agonists; D006801:Humans; D013329:Structure-Activity Relationship; D013872:Thionucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism
chemical_list: C520185:2-chloro-4'-thioadenosine-5'-methyluronamide; D058909:Adenosine A3 Receptor Agonists; D013872:Thionucleosides; D000241:Adenosine; C090034:2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide