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Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders

✍ Scribed by Massimo Gianotti; Corrado Corti; Sonia Delle Fratte; Romano Di Fabio; Colin P. Leslie; Francesca Pavone; Laura Piccoli; Luigi Stasi; Mark J. Wigglesworth

Book ID: 104004641
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 515 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.029

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✦ Synopsis

A novel imidazobenzazepine template (5a) with potent dual H(1)/5-HT(2A) antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R(1)-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]-2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H(1)/5-HT(2A) receptor antagonist activities and good developability profiles.

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