Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders.
Bioorganic & Medicinal Chemistry Letters (2010)
- PubMed: 20674357
Available from linkinghub.elsevier.com
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Abstract
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-imidazo1,2-b2benzazepin-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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