Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596130 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
Starting from a known H4R ligand based on a pyrimidine skeleton, a series of novel analogues based on a pyrrolo[2,3-d]pyrimidine scaffold have been prepared. Whereas the original pyrimidine congener shows good affinity at hH4R (Ki = 0.5 μM), its lacks selectivity with a Ki value for the hH3R of 1 μM. Within the newly synthesized pyrrolo[2,3-d]pyrimidines, several congeners show Ki values of less than 1 μM at the hH4R and show a much improved selectivity profile. Therefore, these series represent an interesting starting point for the discovery of novel hH4R ligands.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ling-Jie Gao, J. Stephan Schwed, Lilia Weizel, Steven De Jonghe, Holger Stark, Piet Herdewijn,