Ontology highlight
ABSTRACT:
SUBMITTER: Bartolome-Nebreda JM
PROVIDER: S-EPMC3924858 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20130904 18
Starting from a singleton chromanone high throughput screening (HTS) hit, we describe a focused medicinal chemistry optimization effort leading to the identification of a novel series of phenoxymethyl-dihydrothiazolopyridone derivatives as selective positive allosteric modulators (PAMs) of the metabotropic glutamate 5 (mGlu5) receptor. These dihydrothiazolopyridones potentiate receptor responses in recombinant systems. In vitro and in vivo drug metabolism and pharmacokinetic (DMPK) evaluation al ...[more]