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New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine
S M Ali1, C E Tedford, R Gregory
1Gliatech Inc., Cleveland, Ohio 44122, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
New histamine H3 receptor antagonists were developed using an acetylene moiety as a replacement for the amide-oxime functionality of verongamine 5. Optimization of receptor binding was performed by following aliphatic Topliss tree guidelines. These new H3 ligands demonstrate excellent blood-brain barrier penetration.