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Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Sep2010, Vol. 20 Issue 17, p5069-5073. 5p. - Publication Year :
- 2010
-
Abstract
- Abstract: A novel imidazobenzazepine template (5a) with potent dual H1/5-HT2A 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-R1-2-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 H1/5-HT2A receptor antagonist activities and good developability profiles. [ABSTRACT FROM AUTHOR]
- Subjects :
- *IMIDES
*HISTAMINE
*SLEEP disorders treatment
*PROPIONIC acid
*TRYPTAMINE
*HYPNOTICS
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 20
- Issue :
- 17
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 52936814
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.07.029