Spirocyclic compounds, potent CCR1 antagonists

N Hossain, S Ivanova, J Bergare, T Eriksson

Index: Hossain, Nafizal; Ivanova, Svetlana; Bergare, Jonas; Eriksson, Tomas Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 6 p. 1883 - 1886

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Citation Number: 6

Abstract

Conformationally constrained spirocycles (17–23) and (31–36) were synthesised. In vitro data revealed that these compounds are CCR1 antagonists with sub-nanomolar potency. In a functional assay 22, 23 and 36 inhibited CCR1 mediated chemotaxis with an IC50 value of 2, 2.6 and 68nM, respectively.