Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold

Wayne D Vaccaro; Rosy Sher; Michael Berlin; Neng-Yang Shih; Robert Aslanian; John H Schwerdt; Kevin D McCormick; John J Piwinski; Robert E West Jr; John C Anthes; Shirley M Williams; Ren-Long Wu; H Susan She; Maria A Rivelli; Jennifer C Mutter; Michel R Corboz; John A Hey; Leonard Favreau

doi:10.1016/j.bmcl.2005.09.076

Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold

Bioorg Med Chem Lett. 2006 Jan 15;16(2):395-9. doi: 10.1016/j.bmcl.2005.09.076. Epub 2005 Oct 21.

Authors

Wayne D Vaccaro¹, Rosy Sher, Michael Berlin, Neng-Yang Shih, Robert Aslanian, John H Schwerdt, Kevin D McCormick, John J Piwinski, Robert E West Jr, John C Anthes, Shirley M Williams, Ren-Long Wu, H Susan She, Maria A Rivelli, Jennifer C Mutter, Michel R Corboz, John A Hey, Leonard Favreau

Affiliation

¹ The Schering Plough Research Institute, 2015 Galloping Hill Rd., Kenilworth, NJ 07033, USA.

PMID: 16246552
DOI: 10.1016/j.bmcl.2005.09.076

Abstract

We report the discovery of novel histamine H(3) receptor antagonists based on 4-[(1H-imidazol-4-yl)methyl]piperidine. The most potent compounds in the series (e.g., 7) result from the attachment of a substituted aniline amide to the main pharmacophore piperidine via a two-methylene linker.

MeSH terms

Cytochrome P-450 CYP2D6 Inhibitors
Drug Evaluation, Preclinical
Histamine Antagonists / chemical synthesis
Histamine Antagonists / chemistry
Histamine Antagonists / pharmacology*
Humans
Imidazoles / chemical synthesis
Imidazoles / chemistry
Imidazoles / pharmacology*
In Vitro Techniques
Molecular Structure
Piperidines / chemical synthesis
Piperidines / chemistry
Piperidines / pharmacology*
Receptors, Histamine H3 / drug effects*
Structure-Activity Relationship

Substances

Cytochrome P-450 CYP2D6 Inhibitors
Histamine Antagonists
Imidazoles
Piperidines
Receptors, Histamine H3
4-(1H-imidazol-4-ylmethyl)piperidine