Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors |
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| Authors: | Andrew F Donnell Paul J Dollings John A Butera Arlene J Dietrich Kerri K Lipinski Afshin Ghavami Warren D Hirst |
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| Institution: | 1. Worldwide Medicinal Chemistry, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USA;2. Neuroscience Research Unit, Pfizer Global Research and Development, CN 8000, Princeton, NJ 08543, USA |
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| Abstract: | Substituted pyridazino4,5-b]indolizines were identified as potent and selective PDE4B inhibitors. We describe the structure–activity relationships generated around an HTS hit that led to a series of compounds with low nanomolar affinity for PDE4B and high selectivity over the PDE4D subtype. |
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