| Literature DB >> 20610153 |
Paul J Coleman1, John D Schreier, Anthony J Roecker, Swati P Mercer, Georgia B McGaughey, Christopher D Cox, George D Hartman, C Meacham Harrell, Duane R Reiss, Scott M Doran, Susan L Garson, Wayne B Anderson, Cuyue Tang, Thomayant Prueksaritanont, Christopher J Winrow, John J Renger.
Abstract
Orexins are excitatory neuropeptides that regulate arousal and sleep. Orexin receptor antagonists promote sleep and offer potential as a new therapy for the treatment of insomnia. In this Letter, we describe the synthesis of constrained diazepanes having a 3,9 diazabicyclo[4.2.1]nonane bicyclic core with good oral bioavailability and sleep-promoting activity in a rat EEG model. 2010 Elsevier Ltd. All rights reserved.Entities:
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Year: 2010 PMID： 20610153 DOI： 10.1016/j.bmcl.2010.05.047
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823