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Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region |
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| Authors: | Hughes Robert O Maddux Todd Joseph Rogier D Lu Sharon Walker John K Jon Jacobsen E Rumsey Jeanne M Zheng Yi Macinnes Alan Bond Brian R Han Seungil |
| Institution: | Pfizer Global Research and Development, 700 Chesterfield Parkway West, St. Louis, MO 63017, USA. robowenhughes@gmail.com |
| Abstract: | 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. |
| Keywords: | PDE5 inhibitors Pyrazinones Lead optimization Ligand efficiency Lipophilic efficiency |
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