Ontology highlight
ABSTRACT:
SUBMITTER: Bartolome-Nebreda JM
PROVIDER: S-EPMC3924858 | biostudies-literature | 2013 Sep
REPOSITORIES: biostudies-literature
Bartolomé-Nebreda José Manuel JM Conde-Ceide Susana S Delgado Francisca F Iturrino Laura L Pastor Joaquín J Pena Miguel Ángel MÁ Trabanco Andrés A AA Tresadern Gary G Wassvik Carola M CM Stauffer Shaun R SR Jadhav Satyawan S Gogi Kiran K Vinson Paige N PN Noetzel Meredith J MJ Days Emily E Weaver C David CD Lindsley Craig W CW Niswender Colleen M CM Jones Carrie K CK Conn P Jeffrey PJ Rombouts Frederik F Lavreysen Hilde H Macdonald Gregor J GJ Mackie Claire C Steckler Thomas T
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]