Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands

doi:10.1016/j.bmcl.2008.08.008

Bioorganic & Medicinal Chemistry Letters

Volume 18, Issue 18, 15 September 2008, Pages 5032-5036

https://doi.org/10.1016/j.bmcl.2008.08.008 Get rights and content

Abstract

A series of non-imidazole histamine H₃ receptor antagonists based on the (3-phenoxypropyl)amine motif, which is a common pharmacophore for H₃ antagonists, has been identified. A preliminary SAR study around the amine moiety has identified 8a as a potent H₃ antagonist possessing a good pharmacokinetic profile in the rat.

Graphical abstract

A series of non-imidazole histamine H₃ receptor antagonists based on the (3-phenoxypropyl)amine motif have been identified. Compound 8a displays a good pharmacokinetic profile in the rat.

Section snippets

Acknowledgments

We thank the Drug Metabolism and Pharmacokinetics group of the Schering-Plough Research Institute, for providing the in vitro and in vivo pharmacokinetic data, and Steve Sorota for providing the hERG data.

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Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands

Abstract

Graphical abstract

Section snippets

Acknowledgments

Drug Discov. Today

Biochem. Pharmacol.

Mol. Interventions

Biochem. Pharmacol.

Expert Opin. Invest. Drugs

Biochem. Pharmacol.

Pharmacology

Drug Metab. Dispos.

Br. J. Pharmacol.

J. Pharm. Sci.

Curr. Allergy Asthma Rep.