Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists

Novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives were identified as potent human H3 receptor inverse agonists. After systematic modification of lead 5a, the potent and selective analog 5r was identified. Elimination of hERG K+ channel and human α1A-adrenoceptor activities is the main focus of the present study.

Graphical abstractA series of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives was discovered as potent human H3 receptor inverse agonists.Figure optionsDownload full-size imageDownload as PowerPoint slide