A new family of H3 receptor antagonists based on the natural product Conessine

Bioorganic & Medicinal Chemistry Letters
Vincent J SantoraAndrew J Grottick

Abstract

A new family of Histamine H(3) receptor antagonists (5a-t) has been prepared based on the structure of the natural product Conessine, a known H(3) antagonist. Several members of the new series are highly potent and selective binders of rat and human H(3) receptors and display inverse agonism at the human H(3) receptor. Compound 5n exhibited promising rat pharmacokinetic properties and demonstrated functional antagonism of the H(3) receptor in an in-vivo pharmacological model.

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Nov 8, 2011·Acta Crystallographica. Section E, Structure Reports Online·Wanwan CaoZhuo Zeng
Dec 2, 2008·Biological & Pharmaceutical Bulletin·Kerstin SanderHolger Stark
Nov 20, 2015·Neuropharmacology·Bassem Sadek, Holger Stark
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Aug 8, 2008·Journal of Medicinal Chemistry·Chen ZhaoMarlon D Cowart
May 31, 2018·Organic Letters·Hua-Chao LiuChun-Jiang Wang

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