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

Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors.

Inhibition of renin enzymatic activity by a series of ketopiperazine-based compounds containing a C6 benzyloxymethyl substituent correlated with a +(pi+sigma) effect. A 3-pyridinyloxymethyl substituent was also found to be equipotent as higher molecular weight analogs, and exhibited decreased CYP3A4 inhibition levels and improved pharmacokinetic properties.[1]

References

  1. Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors. Powell, N.A., Clay, E.H., Holsworth, D.D., Bryant, J.W., Ryan, M.J., Jalaie, M., Edmunds, J.J. Bioorg. Med. Chem. Lett. (2005) [Pubmed]
 
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