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

N Hossain, M Mensonides-Harsema…

Index: Hossain, Nafizal; Mensonides-Harsema, Marguerite; Cooper, Martin E.; Eriksson, Tomas; Ivanova, Svetlana; Bergstroem, Lena Bioorganic and Medicinal Chemistry Letters, 2014 , vol. 24, # 1 p. 108 - 112

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Citation Number: 3

Abstract

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