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Discovery of renin inhibitors containing a simple aspartate binding moiety that imparts reduced P450 inhibition.
Lawhorn BG,
Tran T,
Hong VS,
Morgan LA,
Le BT,
Harpel MR,
Jolivette L,
Diaz E,
Schwartz B,
Gross JW,
Tomaszek T,
Semus S,
Concha N,
Smallwood A,
Holt DA,
Kallander LS
Bioorg Med Chem Lett 27 4838-4843 (2017)
Abstract
Discovery of potent renin inhibitors which contain a simplified alkylamino Asp-binding group and exhibit improved selectivity for renin over Cyp3A4 is described. Structure-function results in this series are rationalized based on analysis of selected compounds bound to renin, and the contribution of each molecular feature leading to the reduced P450 inhibition is quantified.
We are not aware of any publication which cites or mentions this structure.