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Design and Synthesis of N(6)-Substituted-4′-thioadenosine-5′-uronamides As Potent and Selective Human A(3) Adenosine Receptor Agonists

On the basis of a bioisosteric rationale, 4′-thionucleoside analogues of IB-MECA, which is a potent and selective A(3) adenosine receptor agonist (AR), were synthesized from d-gulonic acid γ-lactone. The 4′-thio analogue (5h) of IB-MECA showed extremely high binding affinity (K(i) = 0.25 nM) at the...

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Bibliographic Details
Main Authors: Choi, Won Jun, Lee, Hyuk Woo, Kim, Hea Ok, Chinn, Moshe, Gao, Zhan-Guo, Patel, Amit, Jacobson, Kenneth A., Moon, Hyung Ryong, Jung, Young Hoon, Jeong, Lak Shin
Format: Artigo
Language:Inglês
Published: 2009
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC2797373/
https://ncbi.nlm.nih.gov/pubmed/19879151
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2009.10.011
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