Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part I) | Health & Environmental Research Online (HERO)

Health & Environmental Research Online (HERO)

Print Feedback Export to File

This record has one attached file:

Citation
Tags

HERO ID

7200581

Reference Type

Journal Article

Title

Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part I)

Author(s)

Gao, Z; Hurst, WJ; Guillot, E; Czechtizky, W; Lukasczyk, U; Nagorny, R; Pruniaux, MP; Schwink, L; Sanchez, JA; Stengelin, S; Tang, L; Winkler, I; Hendrix, JA; George, PG; ,

Year

2013

Is Peer Reviewed?

Yes

Journal

Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405

Publisher

PERGAMON-ELSEVIER SCIENCE LTD

Location

OXFORD

Page Numbers

3416-3420

Language

English

PMID

23591110

DOI

10.1016/j.bmcl.2013.03.080

Web of Science Id

WOS:000318976100060

Abstract

A series of structurally novel aryl ureas was derived from optimization of the HTS lead as selective histamine H3 receptor (H3R) antagonists. The SAR was explored and the data obtained set up the starting point and foundation for further optimization. The most potent tool compounds, as exemplified by compounds 2l, 5b, 5d, and 5e, displayed antagonism potencies in the subnanomolar range in in vitro human-H3R FLIPR assays and rhesus monkey H3R binding assays.