| 16143527 |
Powell NA, Clay EH, Holsworth DD, Bryant JW, Ryan MJ, Jalaie M, Edmunds JJ: Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4713-6.
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. |
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