Design, Synthesis, and In Vivo Efficacy of Glycine Transporter‐1 (GlyT1) Inhibitors Derived from a Series of [4‐Phenyl‐1‐(propylsulfonyl)piperidin‐4‐yl]methyl Benzamides

Abstract

An iterative analogue library synthesis approach rapidly delivered (S)-13 h, a potent, reversible, and selective GlyT1 inhibitor. (S)-13 h selectively increased glycine levels in the prefrontal cortex to 340 % of basal levels and significantly enhanced prepulse inhibition in mice. Thereby, providing strong support for the development of novel antipsychotics based on the NMDA hypofunction hypothesis of schizophrenia. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2452/2006/z600097_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.