221310-31-2Relevant articles and documents
New renin inhibitors with hydrophilic C-terminus
Paruszewski,Jaworski,Winiecka,Tautt,Dudkiewicz
, p. 102 - 106 (2007/10/03)
Four new peptide-based renin inhibitors, Boc-Phe(4-OMe)-MePhe-AHPPA- εAhx-EA (11), Boc-Phe(4-OMe)-MeLeu-AHPPA-eAhx-EA (15), Boc-Phe(4-OMe)- MePhe-Sta-εAhx-EA (20) and Boc-Phe(4-OMe)-MeLeu-Sta-εAhx-EA (21) have been synthesized in search of structures with improved biological properties. They were designed as compounds with moderate hydrophobicity (5.28, 4.79, 4.79 and 4.30), respectively. All synthesized inhibitors were resistant to chymotrypsin activity, all were poorly solubile in buffers pH 2.0 and pH 7.4. The inhibitory potency of renin activity in vitro of 11, 15, 20 and 21 expressed as IC50 was 7.0 x 10-4, 7.5 x 10-5, 6.0 x 10-4 and 2.5 x 10-4 M/l, respectively.