| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378569 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
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.
Graphical abstractThe synthesis, SAR, and in vivo characterization of a novel class of CRF1 antagonist are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Y. St-Denis, R. Di Fabio, G. Bernasconi, E. Castiglioni, S. Contini, D. Donati, E. Fazzolari, G. Gentile, D. Ghirlanda, C. Marchionni, F. Messina, F. Micheli, F. Pavone, A. Pasquarello, F.M. Sabbatini, M.G. Zampori, R. Arban, G. Vitulli,