Renin inhibitors containing statine and 6-aminohexanoic acid. Part III
Paruszewski, R.; Tautt, J.; Dudkiewicz, J.
Polish Journal of Pharmacology 45(1): 75-82
1993
ISSN/ISBN: 1230-6002 PMID: 8401762 Document Number: 422481
Five peptide renin inhibitors containing the sequence: Phe-His-Sta-epsilon-Ahx (Sta = 4(S)-amino-3(S)-hydroxy-6-methylheptanoic acid, epsilon-Ahx = 6-aminohexanoic acid) were synthesized and their potency was assayed in vitro by a spectrofluorometric method (assay of Leu-Val-Tyr-Ser released from N-acetyltetradecapeptide substrate by renin in the presence of an inhibitor). Their stability was tested by assay of Phe and Pro-Phe released after incubation with chymotrypsin. The most potent inhibitor was Boc-Phe-His-Sta-epsilon-Ahx-OMe (IC-50 = 5 times 10-9 M/l), the most stable - Boc-Pro-Phe-His-Sta-epsilon-Ahx-OMe (resistant to incubation with chymotrypsin for 4 h).