Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371932 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
Three novel series of histamine H4 receptor (H4R) antagonists containing the 2-aminopyrimidine motif are reported. The best of these compounds display good in vitro potency in both functional and binding assays. In addition, representative compounds are able to completely block itch responses when dosed ip in a mouse model of H4-agonist induced scratching, thus demonstrating their activities as H4R antagonists.
Graphical abstractThree novel series of histamine H4 receptor (H4R) antagonists containing the 2-aminopyrimidine motif are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
John R. Koenig, Huaqing Liu, Irene Drizin, David G. Witte, Tracy L. Carr, Arlene M. Manelli, Ivan Milicic, Marina I. Strakhova, Thomas R. Miller, Timothy A. Esbenshade, Jorge D. Brioni, Marlon Cowart,