| Title : Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP) - Haffner_2008_Bioorg.Med.Chem.Lett_18_4360 |
| Author(s) : Haffner CD , Diaz CJ , Miller AB , Reid RA , Madauss KP , Hassell A , Hanlon MH , Porter DJ , Becherer JD , Carter LH |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :4360 , 2008 |
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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. |
| PubMedSearch : Haffner_2008_Bioorg.Med.Chem.Lett_18_4360 |
| PubMedID: 18606544 |
| Gene_locus related to this paper: human-PREPL |
| Inhibitor | DB07148 |
| Gene_locus | human-PREPL |
| Structure | 3DDU |
Haffner CD, Diaz CJ, Miller AB, Reid RA, Madauss KP, Hassell A, Hanlon MH, Porter DJ, Becherer JD, Carter LH (2008)
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP)
Bioorganic & Medicinal Chemistry Lett
18 :4360
Haffner CD, Diaz CJ, Miller AB, Reid RA, Madauss KP, Hassell A, Hanlon MH, Porter DJ, Becherer JD, Carter LH (2008)
Bioorganic & Medicinal Chemistry Lett
18 :4360