Investigation of the pyrazinones as PDE5 inhibitors: Evaluation of regioisomeric projections into the solvent region
| Autor: | Brian R. Bond, D. Joseph Rogier, Yi Zheng, Maddux Todd Michael, Sharon Lu, Alan MacInnes, Jeanne M. Rumsey, John K. Walker, E. Jon Jacobsen, Robert Hughes, Seungil Han |
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| Rok vydání: | 2011 |
| Předmět: |
Models
Molecular Ligand efficiency Chemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Phosphodiesterase 5 Inhibitors Crystallography X-Ray Biochemistry Combinatorial chemistry Solvent Inhibitory Concentration 50 Lipophilic efficiency Pyrazines Drug Discovery Solvents Molecular Medicine Organic chemistry Inhibitory concentration 50 Selectivity Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:6348-6352 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.08.106 |
| Popis: | We describe the design, synthesis and profiling of a novel series of PDE5 inhibitors. We take advantage of an alternate projection into the solvent region to identify compounds with excellent potency, selectivity and pharmacokinetic profiles. |
| Databáze: | OpenAIRE |
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