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Substituted tetraazaacenaphthylenes as potent CRF1 receptor antagonists for the treatment of depression and anxiety.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 Aug 15; Vol. 15 (16), pp. 3713-6. - Publication Year :
- 2005
-
Abstract
- Two isomers of the hexahydro-tetraazaacenaphthylene templates (1 and 2) are presented as novel, potent, and selective corticotropin releasing factor-1 (CRF1) receptor antagonists. In this paper, we report the affinity and SAR of a series of compounds, as well as pharmacokinetic characterization of a chosen set. The anxiolitic activity of a selected example (2ba) in the rat pup vocalization model is also presented.
- Subjects :
- Acenaphthenes chemical synthesis
Animals
Disease Models, Animal
Drug Evaluation, Preclinical
Molecular Structure
Rats
Rats, Wistar
Structure-Activity Relationship
Acenaphthenes pharmacology
Acenaphthenes therapeutic use
Anxiety drug therapy
Depression drug therapy
Receptors, Corticotropin-Releasing Hormone antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 15
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15946843
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.05.040