Publications by authors named "Theresa A Almos"
Article Synopsis
- * Research shifted to azetidine-based inhibitors, with a notable compound (Compound 26) found to boost cerebrospinal fluid levels of glycine and show similar effectiveness to Bitopertin in rats.
- * Compound 26 also improved memory performance in two behavioral tests after specific doses, indicating its potential as a cognitive enhancer.
We report here the identification and optimization of a novel series of potent GlyT1 inhibitors. A ligand design campaign that utilized known GlyT1 inhibitors as starting points led to the identification of a novel series of pyrrolo[3,4- c]pyrazoles amides (21-50) with good in vitro potency. Subsequent optimization of physicochemical and in vitro ADME properties produced several compounds with promising pharmacokinetic profiles.
View Article and Find Full Text PDF