Synthesis and SAR of novel histamine H3 receptor antagonists

descriptionPublicationkeyboard_double_arrow_right Article 01 Jul 2006 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 16, pages 3,415-3,418 (issn: 0960-894X,

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Authors: Cynthia D, Jesudason; Lisa S, Beavers; Jeffrey W, Cramer; Joelle, Dill; Don R, Finley; Craig W, Lindsley; F Craig, Stevens; +8 Authors

doi: 10.1016/j.bmcl.2006.04.004

pmid: 16677814

Synthesis and SAR of novel histamine H3 receptor antagonists

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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.

Related Organizations

Eli Lilly (United States)
United States

Keywords

Structure-Activity Relationship, Molecular Structure, Tetrahydroisoquinolines, Drug Evaluation, Preclinical, Animals, Humans, Receptors, Histamine H3, Azepines, Rats

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BindingDB Entry 50017774: Synthesis and SAR of novel histamine H3 receptor antagonists.
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