Development of potent and selective human A3 adenosine receptor agonists.
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.
Jeong
Lak Shin
LS
Laboratory of Medicinal Chemistry, College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
Lee
Hyuk Woo
HW
Jacobson
Kenneth A
KA
Lee
Sang Kook
SK
Chun
Moon Woo
MW
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
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