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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

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

doi

10.1016/j.bmcl.2013.03.080

subject

Has Abstract

pub_date

2013-06-01 00:00:00

pages

3416-20

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00408-3

journal_volume

23

pub_type

杂志文章

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