An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes.

Autor: Han X; Pharmaceutical Research Institute, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, USA. xiaojun.han@bms.com, Civiello R, Pin SS, Burris K, Balanda LA, Knipe J, Ren S, Fiedler T, Browman KE, Macci R, Taber MT, Zhang J, Dubowchik GM
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Apr 01; Vol. 17 (7), pp. 2026-30. Date of Electronic Publication: 2007 Jan 13.
DOI: 10.1016/j.bmcl.2007.01.008
Abstrakt: 8-Aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes represent a novel series of high-affinity corticotropin-releasing factor-1 receptor (CRF1R) antagonists. Herein we report the synthesis and SAR around the tricyclic core and the anxiolytic activity of an orally dosed exemplary compound 9d (K(i)=8.0 nM) in a mouse canopy model.
Databáze: MEDLINE