1.
Bioorg Med Chem Lett
; 21(21): 6591-5, 2011 Nov 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21955944
RESUMEN
We describe the identification of a potent, selective lead series that shows antagonism against the human histamine H4 receptor from thirteen actives identified in an HTS as part of a hit to lead program. By focusing on ligand efficiency and concurrently using a diversity based approach, compounds based around 2,4-diaminopyrimidine were identified with compound 25 being quickly shown to be a good lead. It also had the highest ligand efficiency in the series.