The syntheses and biological activities of potent dipeptide renin inhibitors containing a bis[(l-naphthyl)methyl]acetyl group as the N-terminal component are described. ... The renin-angiotensin system is implicated in the regulation of blood pressure. The first and rate-limiting step of the cascade involves the aspartic proteinase renin; therefore, the development of renin inhibitors is expected to provide effective antihypertensive agents. Numerous ...