| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1361967 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The first highly potent and selective PDE8 inhibitors are disclosed. The initial tetrahydroisoquinoline hit was transformed into a nipecotic amide series in order to address a reactive metabolite issue. Reduction of lipophilicity to address metabolic liabilities uncovered an interesting diastereomer-dependent trend in turnover by human microsomes.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael P. DeNinno, Stephen W. Wright, Michael S. Visser, John B. Etienne, Dianna E. Moore, Thanh V. Olson, Benjamin N. Rocke, Melissa P. Andrews, Cynthia Zarbo, Michele L. Millham, Brian P. Boscoe, David D. Boyer, Shawn D. Doran, Karen L. Houseknecht,