ARTICLE: PDF OnlyKokubu T.; Hiwada, K.; Murakami, E.; Muneta, S.; Morisawa, Y.; Yabe, Y.; Koike, H.; Iijima, Y.Journal of Cardiovascular Pharmacology: 1987 - p 88-90 Free Abstract Summary Dipeptide and tripeptide derivatives containing a statine residue were synthesized as human renin inhibitors. ES-305. his(I-naphthyl)methyl acetyl-histidyl-statine-2(S)-methylbutylamide, was found to he a highly potent human renin inhibitor that is species-specific and enzyme-specific. The replacement of the methylhutylamide of ES-305 with the Ieucyl-lysinol (ES-1005) showed similar high potency against human renin (ki value of 2.4 x 10-9M) and monkey renin (Ki value of 7.9 x 10-9M) as ES-305. ES-1005 competitively inhibited human renin. The compound was about one order of magnitude less potent against pig. dog, and rahhit renins. It had moderate inhibitory potencies against cathepsin D and pepsin (IC of cathepsin D) and pepsin of 1.6 x 10-6 and 8.0 x 10-6, M, respectively). ES-1005, a newly synthesized tripeptide derivative containing statine, is a highly potent inhibitor of not only primate renin hut also a wide variety of nonprimate renins. Copyright © 1987 Wolters Kluwer Health, Inc. All rights reserved.