1217315-35-9Relevant academic research and scientific papers
An octahydro-cyclopenta[c]pyrrole series of inhibitors of the type 1 glycine transporter
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
scheme or table, p. 907 - 911 (2010/08/19)
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.
