Structure−Activity Relationships of Truncated d- and l-4′-Thioadenosine Derivatives as Species-Independent A3 Adeno

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• 作者：Lak Shin Jeong ; Shantanu Pal ; Seung Ah Choe ; Won Jun Choi ; Kenneth A. Jacobson ; Zhan-Guo Gao ; Athena M. Klutz ; Xiyan Hou ; Hea Ok Kim ; Hyuk Woo Lee ; Sang Kook Lee ; Dilip K. Tosh ; Hyung Ryong Moon
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：October 23, 2008
• 年：2008
• 卷：51
• 期：20
• 页码：6609-6613
• 全文大小：132K
• 年卷期：v.51,no.20(October 23, 2008)
• ISSN：1520-4804

文摘

Novel d- and l-4′-thioadenosine derivatives lacking the 4′-hydroxymethyl moiety were synthesized, starting from d-mannose and d-gulonic γ-lactone, respectively, as potent and selective species-independent A₃ adenosine receptor (AR) antagonists. Among the novel 4′-truncated 2-H nucleosides tested, a N⁶-(3-chlorobenzyl) derivative 7c was the most potent at the human A₃ AR (K_i = 1.5 nM), but a N⁶-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity.