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1.
Synthesis and SAR of novel histamine H3 receptor antagonists.
Jesudason, Cynthia D; Beavers, Lisa S; Cramer, Jeffrey W; Dill, Joelle; Finley, Don R; Lindsley, Craig W; Stevens, F Craig; Gadski, Robert A; Oldham, Samuel W; Pickard, R Todd; Siedem, Christopher S; Sindelar, Dana K; Singh, Ajay; Watson, Brian M; Hipskind, Philip A.
Bioorg Med Chem Lett ; 16(13): 3415-8, 2006 Jul 01.
Article in English | MEDLINE | ID: mdl-16677814

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.


Subject(s)
Azepines , Receptors, Histamine H3/drug effects , Tetrahydroisoquinolines/chemical synthesis , Animals , Azepines/chemical synthesis , Azepines/chemistry , Azepines/pharmacology , Drug Evaluation, Preclinical , Humans , Molecular Structure , Rats , Structure-Activity Relationship , Tetrahydroisoquinolines/chemistry , Tetrahydroisoquinolines/pharmacology
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