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Synthesis and SAR of novel histamine H3 receptor antagonists

Authors :
Samuel W. Oldham
M. Joelle Dill
Brian Morgan Watson
Craig W. Lindsley
Don Richard Finley
Dana Sindelar
Lisa Selsam Beavers
Cynthia Darshini Jesudason
Philip Arthur Hipskind
Robert Alan Gadski
Ajay Singh
Christopher Stephen Siedem
Jeffrey W Cramer
R. Todd Pickard
F. Craig Stevens
Source :
Bioorganicmedicinal chemistry letters. 16(13)
Publication Year :
2006

Abstract

The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H(3) receptors are described. The substitution around these rings as well as the nature of the substituent on nitrogen is explored. Several compounds with high affinity and selectivity for the human and rat H(3) receptors are reported.

Details

ISSN :
0960894X
Volume :
16
Issue :
13
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.doi.dedup.....0ac411e9c4aa2b7b111ec41de2547f44