New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine

Bioorganic & Medicinal Chemistry Letters
1998.0

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.

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