6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators

József Huszár, József Levente Petró, Zsuzsa Hadady, Amrita Ágnes Bobok,Katalin Sághy, Attila Sándor Halász,Gábor Hornyánszky, Viktor Román,István Greiner, János Éles

Bioorganic & Medicinal Chemistry Letters（2022）

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摘要

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.

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关键词

γ-Aminobutyric acid,GABA,GABAB receptor,Positive allosteric modulators,PAMs

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