Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP)
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.
Haffner, Curt D.,Diaz, Caroline J.,Miller, Aaron B.,Reid, Robert A.,Madauss, Kevin P.,Hassell, Annie,Hanlon, Mary H.,Porter, David J.T.,Becherer, J. David,Carter, Luke H.
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p. 4360 - 4363
(2009/04/06)
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