161670-35-5

Upstream product

• 35026-08-5 N-methyl-L-leucine methyl ester 
• 53267-93-9 O-methyl-N-tert-butoxycarbonyl-L-tyrosine 
• 130994-88-6 methyl N-methyl-N-(tert-butoxycarbonyl)-L-leucinate 
• 53363-89-6 N-t-butoxycarbonyl-N-methyl-L-leucine 

Downstream Products

• 161670-36-6 Boc-Phe(4-OMe)-MeLeu-OH 
• 189162-94-5 (3S,4S)-4-((S)-2-{[(S)-2-Amino-3-(4-methoxy-phenyl)-propionyl]-methyl-amino}-4-methyl-pentanoylamino)-3-hydroxy-6-methyl-heptanoic acid [5-(3-methyl-butylcarbamoyl)-pentyl]-amide 
• 161670-37-7 [(S)-1-{[(S)-1-((S)-1-{(S)-1-Hydroxy-2-[5-(3-methyl-butylcarbamoyl)-pentylcarbamoyl]-ethyl}-3-methyl-butylcarbamoyl)-3-methyl-butyl]-methyl-carbamoyl}-2-(4-methoxy-phenyl)-ethyl]-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

New renin inhibitors containing pseudodipeptidic units in P 3-P2 and P1-P1′ positions

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 with hydrophilic C-terminus

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.

New renin inhibitors containing aliphatic or aromatic amides at the C-terminus

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.