Sm. Ali et al., NEW ACETYLENE BASED HISTAMINE H-2-RECEPTOR ANTAGONISTS DERIVED FROM THE MARINE NATURAL PRODUCT VERONGAMINE, Bioorganic & medicinal chemistry letters, 8(10), 1998, pp. 1133-1138
New histamine H-3 receptor antagonists were developed using an acetyle
ne moiety as a replacement or the amide-oxime functionality of veronga
mine 5. Optimization of receptor binding was performed by following al
iphatic Topliss tree guidelines. These new H-3 ligands demonstrate exc
ellent blood-brain barrier penetration. (C) 1998 Elsevier Science Ltd.
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