Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).
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Haffner CD, Diaz CJ, Miller AB, Reid RA, Madauss KP, Hassell A, Hanlon MH, Porter DJ, Becherer JD, Carter LH
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).
Bioorg Med Chem Lett. 2008 Aug 1;18(15):4360-3. doi: 10.1016/j.bmcl.2008.06.067. Epub 2008 Jun 24.
- PubMed ID
- 18606544 [ View in PubMed]
- Abstract
We report the synthesis and in vitro activity of a series of novel pyrrolidinyl pyridones and pyrazinones as potent inhibitors of prolyl oligopeptidase (POP). Within this series, compound 39 was co-crystallized within the catalytic site of a human chimeric POP protein which provided a more detailed understanding of how these inhibitors interacted with the key residues within the catalytic pocket.