Bioorganic and Medicinal Chemistry Letters p. 3713 - 3716 (2005)
Update date:2022-07-31
Topics:
St.-Denis
Di Fabio
Bernasconi
Castiglioni
Contini
Donati
Fazzolari
Gentile
Ghirlanda
Marchionni
Messina
Micheli
Pavone
Pasquarello
Sabbatini
Zampori
Arban
Vitulli
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.
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Doi:10.1016/S0960-894X(00)00262-6
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(2003)