Title of article :
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists
Author/Authors :
Takashi Mizutani، نويسنده , , Tsuyoshi Nagase، نويسنده , , Sayaka Ito، نويسنده , , Yasuhisa Miyamoto، نويسنده , , Takeshi Tanaka، نويسنده , , Norihiro Takenaga، نويسنده , , Shigeru Tokita، نويسنده , , Nagaaki Sato، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Abstract :
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.
Keywords :
?1A-Adrenoceptor , Quinazolinone , Histamine release assay , hERG K+ channel , Histamine H3 receptor inverse agonists
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
