Structure− activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands

…, BM Bettencourt, LA Black, SR Fix-Stenzel…

Index: Altenbach, Robert J.; Adair, Ronald M.; Bettencourt, Brian M.; Black, Lawrence A.; Fix-Stenzel, Shannon R.; Gopalakrishnan, Sujatha M.; Hsieh, Gin C.; Liu, Huaqing; Marsh, Kennan C.; McPherson, Michael J.; Milicic, Ivan; Miller, Thomas R.; Vortherms, Timothy A.; Warrior, Usha; Wetter, Jill M.; Wishart, Neil; Witte, David G.; Honore, Prisca; Esbenshade, Timothy A.; Hancock, Arthur A.; Brioni, Jorge D.; Cowart, Marlon D. Journal of Medicinal Chemistry, 2008 , vol. 51, # 20 p. 6571 - 6580

Full Text: HTML

Citation Number: 63

Abstract

A series of 2-aminopyrimidines was synthesized as ligands of the histamine H4 receptor (H4R). Working in part from a pyrimidine hit that was identified in an HTS campaign, SAR studies were carried out to optimize the potency, which led to compound 3, 4-tert-butyl-6-(4- methylpiperazin-1-yl) pyrimidin-2-ylamine. We further studied this compound by systematically modifying the core pyrimidine moiety, the methylpiperazine at position 4, ...