1. Synthesis and SAR of novel histamine H3 receptor antagonists
- Author
-
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, and F. Craig Stevens
- Subjects
Stereochemistry ,Clinical Biochemistry ,Substituent ,Drug Evaluation, Preclinical ,Pharmaceutical Science ,Biochemistry ,Chemical synthesis ,chemistry.chemical_compound ,Structure-Activity Relationship ,Tetrahydroisoquinolines ,Drug Discovery ,Structure–activity relationship ,Animals ,Humans ,Receptors, Histamine H3 ,Receptor ,Molecular Biology ,Molecular Structure ,Tetrahydroisoquinoline ,Organic Chemistry ,Biological activity ,Azepines ,Rats ,chemistry ,Molecular Medicine ,Histamine H3 receptor ,Selectivity - 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.
- Published
- 2006