1383718-75-9Relevant academic research and scientific papers
Discovery, synthesis, and structure-activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators
Kubas, Holger,Meyer, Udo,Krueger, Bjoern,Hechenberger, Mirko,Vanejevs, Maksims,Zemribo, Ronalds,Kauss, Valerjans,Ambartsumova, Raisa,Pyatkin, Ilya,Polosukhin, Alexey I.,Abel, Ulrich
supporting information, p. 4493 - 4500 (2013/08/23)
A virtual screening approach using various in silico methodologies led to the discovery of 2-(m-tolylamino)-7,8-dihydroquinazolin-5(6H)-one (1) as a moderately active negative allosteric modulator (NAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) showing high selectivity against the subtype mGluR1. Modifications of the parent compound by rational design yielded a series of highly potent derivatives which will serve as valuable starting points for further hit-to-lead optimization efforts toward a suitable drug candidate for the treatment of l-DOPA induced dyskinesia.
METABOTROPIC GLUTAMATE RECEPTOR MODULATORS
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Page/Page column 61, (2012/07/13)
The invention relates to heterocyclic derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are mGluR5 modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorder
