| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369191 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zhongli Gao, William J. Hurst, Etienne Guillot, Werngard Czechtizky, Ulrike Lukasczyk, Raisa Nagorny, Marie-Pierre Pruniaux, Lothar Schwink, Juan Antonio Sanchez, Siegfried Stengelin, Lei Tang, Irvin Winkler, James A. Hendrix, Pascal G. George,