Bioorganic and Medicinal Chemistry Letters p. 2735 - 2740 (1997)
Update date:2022-08-03
Topics:
Goeschke, Richard
Cohen, Nissim Claude
Wood, Jeanette M.
Maibaum, Juergen
Novel low-molecular weight transition-state peptidomimetic renin inhibitors characterized by an all-carbon 8-phenyl substituted octanecarboxamide skeleton have been discovered based on a topographical design approach. The in vitro most potent inhibitors 21, 25 and 26 incorporating a strong H-bond acceptor group linked to the benzyl spacer of the (P3-P1)-unit had IC50s in the low nanomolar range against human renin.
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