Bioorganic and Medicinal Chemistry Letters p. 907 - 911 (2010)
Update date:2022-09-26
Topics:
Lowe III, John A.
DeNinno, Shari L.
Drozda, Susan E.
Schmidt, Christopher J.
Ward, Karen M.
David Tingley III
Sanner, Mark
Tunucci, Don
Valentine, James
We describe a novel series of inhibitors of the type 1 glycine transporter (GlyT1) as an approach to relieving the glutamatergic deficit that is thought to underlie schizophrenia. Synthesis and SAR follow-up of a series of octahydro-cyclopenta[c]pyrrole derivatives afforded potent in vitro inhibition of GlyT1 as well as in vivo activity in elevating CSF glycine. We also found that a 3-O(c-pentyl), 4-F substituent may serve as a surrogate for the widely used 3-trifluoromethoxy group, suggesting its application as an isostere for future medicinal chemistry studies.
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