AI Article Synopsis
- A new series of PDE2 inhibitors was developed and optimized for better activity and reduced side effects.
- Compound 4, the top candidate, showed enhanced cognitive function in both rats and non-human primates during specific tasks.
- Structural studies of a similar compound helped clarify how it selectively binds to the PDE2 enzyme, offering insights into its effectiveness.
Article Abstract
An internal HTS effort identified a novel PDE2 inhibitor series that was subsequently optimized for improved PDE2 activity and off-target selectivity. The optimized lead, compound 4, improved cognitive performance in a rodent novel object recognition task as well as a non-human primate object retrieval task. In addition, co-crystallization studies of close analog of 4 in the PDE2 active site revealed unique binding interactions influencing the high PDE isoform selectivity.
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| http://dx.doi.org/10.1016/j.bmcl.2018.01.039 | DOI Listing |
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