- Acylglycinamides as inhibitors of glycine transporter type 1.
Acylglycinamides as inhibitors of glycine transporter type 1.
Bioorganic & medicinal chemistry letters (2011-09-06)
Richard Blunt, Roderick Porter, Amanda Johns, David Nash, Gemma Puckey, Paul Wyman, Hugh Herdon, Simon Teague, Victoria Hadden, Stefano Fontana, Laurie Gordon
PMID21889344
ABSTRACT
A screening hit was used as the basis for the core structure of a new series of acylglycinamide GlyT-1 inhibitors. Investigation of the SAR around four areas of diversity used facile chemistry to prepare compounds quickly. By focussing on reducing the lipophilicity and improving the aqueous solubility in the series we were able to prepare a compound (17e) with a good level of activity at GlyT-1, selectivity over GlyT-2 and moderate oral bioavailability.