Ontology highlight
ABSTRACT:
SUBMITTER: Malosh C
PROVIDER: S-EPMC4634704 | biostudies-literature | 2015 Nov
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20151009 22
We report the optimization of a series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from an acyl dihydropyrazolo[1,5-a]pyrimidinone class. Investigation of exocyclic amide transpositions with this unique 5,6-bicyclic core were conducted in attempt to modulate physicochemical properties and identify a suitable backup candidate with a reduced half-life. A potent and selective PAM, 1-(2-(phenoxymethyl)-6,7-dihydropyrazolo[1,5-a]pyrimidin-4(5H)-yl)ethanone (9a, ...[more]