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ID: ALA3098005

Journal: Bioorg Med Chem Lett

Title: Structure activity relationships of fused bicyclic and urea derivatives of spirocyclic compounds as potent CCR1 antagonists.

Authors: Hossain N, Mensonides-Harsema M, Cooper ME, Eriksson T, Ivanova S, Bergström L.

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 (7nM), 44 (1.3nM), 48 (0.89nM) and 50 (0.63nM) 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 16nM.

CiteXplore: 24332486

DOI: 10.1016/j.bmcl.2013.11.062