In order to find specific renin inhibitors, various kinds of oligopeptide derivatives were synthesized, which have amino acid sequences identical with or analogous to the partial structure of angiotensinogen around the renin attacking site, the Leu10-Leu11 bond. Among the 20 tetra-, penta-, and octa-peptide derivatives tested for the inhibitory activity on the renin-angiotensin system, eight compounds were found to be active, all of which have the Leu-Leu bond in their molecules. Some structure-activity relationship is discussed on the basis of the present work and the results of preceding work.