An introduction of a pyridine group into the structure of prolyl oligopeptidase inhibitors |
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Authors: | Jarho Elina M Venäläinen Jarkko I Juntunen Juha Yli-Kokko A Leena Vepsäläinen Jouko Christiaans Johannes A M Forsberg Markus M Järvinen Tomi Männistö Pekka T Wallén Erik A A |
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Affiliation: | Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FI-70211 Kuopio, Finland. Elina.Jarho@uku.fi |
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Abstract: | A series of ionizable prolyl oligopeptidase inhibitors were developed through the introduction of a pyridyl group to the P3 position of the prolyl oligopeptidase inhibitor structure. The study was performed on previously developed prolyl oligopeptidase inhibitors with proline mimetics at the P2 position. The 3-pyridyl group resulted in equipotent compounds as compared to the parent compounds. It was shown that the pyridyl group improves water solubility and, in combination with a 5(R)-tert-butyl-l-prolyl group at the P2 position, good lipophilicity can be achieved. |
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