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Novel substituted tetrahydrotriazaacenaphthylene derivatives as potent CRF1 receptor antagonists.

Abstract：

:Corticotropin-releasing factor (CRF), a 41 amino acid peptide neurohormone synthesised by specific hypothalamic nuclei in the brain, is implicated in stress-related function. Antagonism of CRF(1) receptors is an attractive therapeutic approach for the treatment of depression and anxiety. Unsaturated tetrahydrotriazaacenaphthylenes of general structure 3 have been identified as potent and selective CRF(1) receptor antagonists with a suitable oral pharmacokinetic profile.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gentile G,Di Fabio R,Pavone F,Sabbatini FM,St-Denis Y,Zampori MG,Vitulli G,Worby A

doi

10.1016/j.bmcl.2007.06.077

subject

Has Abstract

pub_date

2007-09-15 00:00:00

pages

5218-21

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00772-X

journal_volume

17

pub_type

杂志文章

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