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Conde-Ceide S.,Neuroscience Medicinal Chemistry | Martinez-Viturro C.M.,Neuroscience Medicinal Chemistry | Alcazar J.,Discovery science Lead Discovery | Garcia-Barrantes P.M.,Vanderbilt University | And 11 more authors.
ACS Medicinal Chemistry Letters | Year: 2015

Herein, we report the structure-activity relationship of a novel series of (2(phenoxymethyl)-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-yl(aryl)methanones as potent, selective, and orally bioavailable metabotropic glutamate receptor subtype 5 (mGlu5) positive allosteric modulators (PAMs). On the basis of its robust in vitro potency and in vivo efficacy in multiple preclinical models of multiple domains of schizophrenia, coupled with a good DMPK profile and an acceptable therapeutic window, 17a (VU0409551/JNJ-46778212) was selected as a candidate for further development. © 2015 American Chemical Society.

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