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.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2013.03.080 | DOI Listing |
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!