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ID: ALA1124786

Journal: J Med Chem

Title: Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.

Authors: Rosenberg SH, Dellaria JF, Kempf DJ, Hutchins CW, Woods KW, Maki RG, de Lara E, Spina KP, Stein HH, Cohen J.

Abstract: A series of low-nanomolar renin inhibitors containing novel C-terminal heterocycles has been designed by formally cyclizing the C-terminus of a glycol-based inhibitor to the second hydroxyl. Molecular modeling suggests that the heterocyclic oxygen hydrogen bonds as an acceptor to the flap region of renin and that the second hydroxyl in the glycol-based inhibitors behaves similarly.

CiteXplore: 2187994

DOI: 10.1021/jm00168a009