Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders |
| |
| Authors: | Massimo Gianotti Corrado Corti Sonia Delle Fratte Romano Di Fabio Colin P Leslie Francesca Pavone Laura Piccoli Luigi Stasi Mark J Wigglesworth |
| |
| Institution: | 1. Neurosciences CEDD, GlaxoSmithKline, Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy;2. GlaxoSmithKline Medicines Research Centre, NFSP, Harlow, UK |
| |
| 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-imidazo1,2-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. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
