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 A©ýAdenosine Receptor Antagonists©ö
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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 ¥ã-lactone, respectively, as potent and selective species-independent A©ý 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 A©ý 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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