Fragment based design of new H4 receptor− ligands with anti-inflammatory properties in vivo

…, G Coruzzi, R Leurs, IJP de Esch

文献索引：Smits, Rogier A.; Lim, Herman D.; Stegink, Bart; Bakker, Remko A.; De Esch, Iwan J. P.; Leurs, Rob Journal of Medicinal Chemistry, 2006 , vol. 49, # 15 p. 4512 - 4516

全文：HTML全文

被引用次数: 107

摘要

Using a previously reported flexible alignment model we have designed, synthesized, and evaluated a series of compounds at the human histamine H4 receptor (H4R) from which 2-(4- methyl-piperazin-1-yl)-quinoxaline (3) was identified as a new lead structure for H4R ligands. Exploration of the structure− activity relationship (SAR) of this scaffold led to the identification of 6, 7-dichloro 3-(4-methylpiperazin-1-yl) quinoxalin-2 (1 H)-one (VUF ...