title: Synthesis of N6-substituted 3'-ureidoadenosine derivatives as highly potent agonists at the mutant A3 adenosine receptor.
abstract: Several N6-substituted 3 '-ureidoadenosine derivatives were efficiently synthesized starting from D-glucose for the development of H272E mutant A3 adenosine receptor (AR) agonists. Among compounds tested, 3 '-ureido-N6-(3-iodobenzyl)adenosine (2c) exhibited the highest binding affinity (Ki = 0.22 micro M) at the H272E mutant A3 AR without binding to the natural A3AR.
authors: College of Pharmacy, Ewha Womans University, Seoul, Korea. lakjeong@ewha.ac.kr
authors: Lak Shin
authors: LS
authors: Jeong
authors: Seung Ah
authors: SA
authors: Choe
authors: Ae Yil
authors: AY
authors: Kim
authors: Hea Ok
authors: HO
authors: Kim
authors: Zhan-Guo
authors: ZG
authors: Gao
authors: Kenneth A
authors: KA
authors: Jacobson
authors: Moon Woo
authors: MW
authors: Chun
authors: Hyung Ryong
authors: HR
authors: Moon
mesh_terms: D058909:Adenosine A3 Receptor Agonists; D003839:Deoxyadenosines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D050505:Mutant Proteins / Q000819:agonists*; D009584:Nitrogen / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D058909:Adenosine A3 Receptor Agonists; D003839:Deoxyadenosines; D050505:Mutant Proteins; D009584:Nitrogen