Synthesis and SAR of novel histamine H sub(3) receptor antagonists

Synthesis and SAR of novel histamine H sub(3) receptor antagonists

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

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (13), p.3415-3418
Hauptverfasser: Jesudason, Cynthia D, Beavers, Lisa S, Cramer, Jeffrey W, Dill, Joelle, Finley, Don R, Lindsley, Craig W, Stevens, FCraig, Gadski, Robert A, Oldham, Samuel W, Pickard, RTodd, Siedem, Christopher S, Sindelar, Dana K, Singh, Ajay, Watson, Brian M, Hipskind, Philip A
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Sprache:eng
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Zusammenfassung:The synthesis and biological evaluation of novel tetrahydroisoquinoline, tetrahydroquinoline, and tetrahydroazepine antagonists of the human and rat H sub(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 sub(3) receptors are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.04.004