Elucidation of fluorine's impact on pKa and in vitro Pgp-mediated efflux for a series of PDE9 inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "MedChemComm"
DOI: 10.1039/c8md00114f
Abstract: P-Glycoprotein (Pgp)-mediated cellular efflux is recognized as a common challenge in CNS drug discovery. In this study, the influence of replacing a hydrogen atom with fluorine on the pKa and Pgp-mediated efflux is elucidated for… read more here.
Keywords: series pde9; pgp mediated; pka; mediated efflux ... See more keywords
Computational Study on Selective PDE9 Inhibitors on PDE9-Mg/Mg, PDE9-Zn/Mg, and PDE9-Zn/Zn Systems
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DOI: 10.3390/biom11050709
Abstract: PDE9 inhibitors have been studied to validate their potential to treat diabetes, neurodegenerative disorders, cardiovascular diseases, and erectile dysfunction. In this report, we have selected highly potent previously reported selective PDE9 inhibitors BAY73-6691R, BAY73-6691S, 28r,… read more here.
Keywords: pde9 pde9; computational study; selective pde9; study selective ... See more keywords