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KMID : 0617320080190010027
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Journal of Pharmacetical Sceiences Ewha Womans University
2008 Volume.19 No. 1 p.27 ~ p.31
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Structure-Activity Relationships of Truncated D- and L-4´-Thioadenosine Derivatives as Species-Independent A₃Adenosine Receptor Antagonists¹
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Jeong Lak-Shin
Pal Shantanu
Choe Seung-Ah
Choi Won-Jun
Jacobson Kenneth A.
Gao Zhan-Guo
Klutz Athena M.
Hou Xiyan
Kim Hea-Ok
Lee Sang-Kook
Tosh Dilip K.
Moon Hyung-Ryong
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Abstract
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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 N^(6)-(3-chlorobenzyl) derivative 7c was the most potent at the human A₃ AR (K_(i) = 1.5 nM), but a N^(6)-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity.
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