6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators. (1st July 2022)

• Record Type: Journal Article
• Authors: Huszár, József; Petró, József Levente; Hadady, Zsuzsa; Bobok, Amrita Ágnes; Sághy, Katalin; Halász, Attila Sándor; Hornyánszky, Gábor; Román, Viktor; Greiner, István; Éles, János
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 67(2022)
• Publication Date: 2022-07-01
• Subjects: γ-Aminobutyric acid -- GABA -- GABAB receptor -- Positive allosteric modulators -- PAMs; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2022.128714
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.