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3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists

Authors :
Zhao, Shu-Hai
Berger, Jacob
Clark, Robin D.
Sethofer, Steven G.
Krauss, Nancy E.
Brothers, Julie M.
Martin, Renee S.
Misner, Dinah L.
Schwab, Dietmar
Alexandrova, Ludmila
Source :
Bioorganic & Medicinal Chemistry Letters. Jun2007, Vol. 17 Issue 12, p3504-3507. 4p.
Publication Year :
2007

Abstract

Abstract: A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT6 receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT6 receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
17
Issue :
12
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
25342271
Full Text :
https://doi.org/10.1016/j.bmcl.2006.12.093