| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367083 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
A series of new selective, high affinity A1-AdoR agonists is reported. Compound 23 that incorporated a carboxylic acid functionality in the 4-position of the pyrazole ring displayed KiL value of 1 nM for the A1-AdoR and >5000-fold selectivity over the A3 and A2A-AdoRs. In addition, compound 19 that incorporated a carboxamide functionality in the 4-position of the pyrazole ring displayed subnanomolar affinity for the A1-AdoR (KiL = 0.6 nM) and >600-fold selectivity over the A3 and A2A-AdoRs.
Graphical abstractThe synthesis, binding affinity and selectivity of 2,6-disubstituted adenosine derivatives for the A1-AdoR is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Elfatih Elzein, Rao Kalla, Xiaofen Li, Thao Perry, Tim Marquart, Mark Micklatcher, Yuan Li, Yuzhi Wu, Dewan Zeng, Jeff Zablocki,