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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

The Discovery of Tropane-derived CCR5 Receptor Antagonists.

The development of compound 1, a piperidine-based CCR5 receptor antagonist with Type I CYP2D6 inhibition, into the tropane-derived analogue 5, is described. This compound, which is devoid of CYP2D6 liabilities, is a highly potent ligand for the CCR5 receptor and has broad-spectrum activity against a range of clinically relevant HIV isolates. The identification of human ether a-go-go-related gene channel inhibition within this series is described and the potential for QTc interval prolongation discussed. Furthermore, structure activity relationship (SAR) around the piperidine moiety is also described.[1]

References

  1. The Discovery of Tropane-derived CCR5 Receptor Antagonists. Armour, D.R., de Groot, M.J., Price, D.A., Stammen, B.L., Wood, A., Perros, M., Burt, C. Chemical biology & drug design. (2006) [Pubmed]
 
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