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2004
Nucleic acids
U 0700
Structure—Affinity Relationships of 5'-Aromatic Ethers and 5'-Aromatic Sulfides
Partial A1 Adenosine Agonists, Potential Supraventricular anti-Arrhythmic
47- 192 as
Agents. — Analogues of the full adenosine receptor agonist tecadenoson incorporating
an 5'-aromatic ether or sulfide are synthesized via the Mitsunobu coupling reaction
starting from tecadenoson. 5'-Modified adenosine derivatives (I) are partial agonists
with respect to their atrioventricular nodal effects. Moderate GTPγS binding values are
observed for (I), suggesting the partial activity. Both compounds show reasonable pharmacokinetic profiles relative to adenosine. — (MORRISON*, C. F.; et al.; Bioorg.
Med. Chem. Lett. 14 (2004) 14, 3793-3797; Dep. Bioorg. Chem., CV Therapeutics
Inc., Palo Alto, CA 94304, USA; Eng.) — H. Hoennerscheid
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