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Synthesis and SAR of novel histamine H3 receptor antagonists |
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| Authors: | 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 |
| Institution: | Lilly Research Laboratories, Eli Lilly & Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. jesudason_cynthia_d@lilly.com |
| 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. |
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