161670-35-5Relevant articles and documents
New renin inhibitors containing pseudodipeptidic units in P 3-P2 and P1-P1′ positions
Paruszewski, Ryszard,Jaworski, Pawel,Bodnar, Magdalena,Dudkiewicz-Wilczynska, Jadwiga,Roman, Iza
, p. 1305 - 1309 (2007/10/03)
A series of four non-peptidic renin inhibitors have been designed and synthesized. All of them contain in their molecule (3S,4S)-4-amino-5-cyclohexyl- 3-hydroxypentanoic acid (ACHPA), a hydrophobic portion at the C-terminus and a second dipeptide-like tra
New renin inhibitors containing aliphatic or aromatic amides at the C-terminus
Paruszewski,Jaworski,Tautt,Dudkiewicz
, p. 206 - 209 (2007/10/03)
Five renin inhibitors, Iva-Pro-Phe(4-OMe)-MeLeu-Sta-εAhx-IAA (18), Iva-εAhx-Phe(4-OMe)-MeLeu-Sta-εAhx-IAA (23), H-εAhx-Phe(4-OMe)-His-Sta-εAhx-FBZA (36), H-εAhx-Phe(4-OMe)-His-Sta-εAhx-MBZA (45), and H-Phe (4-OMe)-His-Sta-εAhx-FBZA (48) have been synthesized in search of structures of improved biological properties. All synthesized inhibitors were resistant to chymotrypsin activity. Inhibitors 18 and 23 were insoluble in buffers, pH 7.4 and 2.0, 36, 45 and 48 were very good soluble in buffer pH 2.0 and poorly in buffer pH 7.4. Experimentally determined 1-octanol/pH 7.4 buffer partition coefficients (log P) of 36, 45 and 48 were above 1. Log P values of 18, 23, 36, 45 and 48 were 6.57, 6.91, 2.48, 2.09 and 2.00 respectively. The inhibitory potency in vitro of 18, 23, 36, 45 and 48 expressed as IC50 was 7.5 · 10-5, 5.0 · 10-6, 7.5 · 10-3, 1.0 · 10-4 and 2.5 · 10-5 M/l respectively.