6-Aryl-quinazolines as novel GABA<sub>B</sub> receptor positive allosteric modulators.

Basic Information

ID: ALA5120808

Journal: Bioorg Med Chem Lett

Title: 6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators.

Authors: Huszár J, Petró JL, Hadady Z, Bobok AÁ, Sághy K, Halász AS, Hornyánszky G, Román V, Greiner I, Éles J.

Abstract: The systemic use of GABAB orthosteric agonist baclofen might be limited due to its detrimental properties: sedation and motor impairment. In contrast, GABAB positive allosteric modulators produce less adverse effects. Using BHF-177 as a starting point, we found a new active scaffold: the 6-aryl-quinazoline scaffold. Further elaborating the scaffold, we identified several in vitro and in vivo active compounds.

CiteXplore: 35367591

DOI: 10.1016/j.bmcl.2022.128714

Patent ID: