基于4-[(1H-咪唑-4-基)甲基]哌啶骨架的新型组胺H3受体拮抗剂。

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

作者信息

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

机构信息

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

出版信息

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

DOI:10.1016/j.bmcl.2005.09.076

PMID:16246552

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.

摘要

我们报道了基于4-[(1H-咪唑-4-基)甲基]哌啶发现新型组胺H(3)受体拮抗剂。该系列中最具活性的化合物（如化合物7）是通过一个二亚甲基连接基将取代苯胺酰胺连接到主要药效基团哌啶上得到的。