Triazole ligands reveal distinct molecular features that induce histamine H4 receptor affinity and subtly govern H4/H3 subtype selectivity

…, O Zuiderveld, IJP de Esch, R Leurs

文献索引：Lim, Herman D.; Smits, Rogier A.; Bakker, Remko A.; Van Dam, Cindy M. E.; De Esch, Iwan J. P.; Leurs, Rob Journal of Medicinal Chemistry, 2006 , vol. 49, # 23 p. 6650 - 6651

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被引用次数: 31

摘要

The histamine H3 (H3R) and H4 (H4R) receptors attract considerable interest from the medicinal chemistry community. Given their relatively high homology yet widely differing therapeutic promises, ligand selectivity for the two receptors is crucial. We interrogated H4R/H3R selectivities using ligands with a [1, 2, 3] triazole core. Cu (I)-assisted “click chemistry” was used to assemble diverse [1, 2, 3] triazole compounds (6a− w and 7a− f), ...