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

…, Y Miyamoto, T Tanaka, N Takenaga, S Tokita…

Index: Mizutani, Takashi; Nagase, Tsuyoshi; Ito, Sayaka; Miyamoto, Yasuhisa; Tanaka, Takeshi; Takenaga, Norihiro; Tokita, Shigeru; Sato, Nagaaki Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 23 p. 6041 - 6045

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Citation Number: 24

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.