Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592757 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
A series of fused bicyclic and urea derivatives of spirocyclic compounds were designed, synthesised and evaluated in vitro as potent CCR1 antagonists. In particular, 4 (7Â nM), 44 (1.3Â nM), 48 (0.89Â nM) and 50 (0.63Â nM) were the most potent hCCR1 antagonists in this series of compounds. Moreover, some of these substances demonstrated good rodent cross-over, especially 46 which exhibited very high rat CCR1 binding affinity with an IC50 value of 16Â nM.
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Authors
Nafizal Hossain, Marguérite Mensonides-Harsema, Martin E. Cooper, Tomas Eriksson, Svetlana Ivanova, Lena Bergström,