Structure–activity relationships of adenosines with heterocyclic N 6-substituents

…, SP Baker, CH Schiesser, PJ Scammells

文献索引：Ashton; Aumann, Kylee M.; Baker, Stephen P.; Schiesser, Carl H.; Scammells, Peter J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 24 p. 6779 - 6784

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被引用次数: 25

摘要

Two series of N6-substituted adenosines with monocyclic and bicyclic N6 substituents containing a heteroatom were synthesized in good yields. These derivatives were assessed for their affinity ([3H] CPX), potency, and intrinsic activity (cAMP accumulation) at the A1 adenosine receptor in DDT1 MF-2 cells. In the monocyclic series, the N6-tetrahydrofuran-3- yl and thiolan-3-yl adenosines (1 and 26, respectively) were found to possess similar ...