865469-49-4

Upstream product

• 13726-69-7 (2S,4R)-4-hydroxy-1-[(2-methylpropan-2-yl)oxycarbonyl]pyrrolidine-2-carboxylic acid 
• 89813-47-8 N-(tert-butoxycarbonyl)-(2S,4R)-4-hydroxyproline benzyl ester 
• 1219136-27-2 (2S,4S)-2-benzyl 1-tert-butyl 4-iodopyrrolidine-1,2-dicarboxylate 
• 51-35-4 4R-4-hydroxyproline 
• 24424-99-5 di-tert-butyl dicarbonate 
• 100-39-0 benzyl bromide 
• 51154-06-4 (S)-2,5-dihydropyrrole-1,2-dicarboxylic acid 1-tert-butyl ester 

Downstream Products

• 178267-93-1 (5S,9R,12S,15S,17aS)-5,15-Diethyl-12-hydroxymethyl-9-phenyl-3,5,6,9,10,12,13,15,16,17a-decahydro-8H-3a,6,10,13,16-pentaaza-cyclopentacyclohexadecene-4,7,11,14,17-pentaone 
• 865469-50-7 N-(tert-Butoxycarbonyl)-(2S,3R,4S)-3,4-dihydroxyproline benzyl ester 
• 35889-87-3 1H-pyrrole-2-carboxylic acid benzyl ester 
• 668987-22-2 2-hydroxyethyl 1H-pyrrole-2-carboxylate 

Relevant academic research and scientific papers

Design and synthesis of plant cyclopeptide Astin C analogues and investigation of their immunosuppressive activity

To further investigate on the structure-activity relationships of immunosuppressive Astin C, seventeen analogues 1–17 were designed and synthetized via amino acid substitution strategy by the solid-phase peptide synthesis method for the first time. In comparison with Astin C (IC50 = 12.6 ± 3.3 μM), only compounds 2 (IC50 = 38.4 ± 16.2 μM), 4 (IC50 = 51.8 ± 12.7 μM), 5 (IC50 = 65.2 ± 15.6 μM), and 8 (IC50 = 61.8 ± 12.4 μM) exhibited immunosuppressive activity in the Lymph node cells of mice. These results showed that the Astin C analogues containing D-amino acid residues, hydrophobic long-chain alkyl substituents, and aryl substituents performed better than those carrying hydrophilic amino acid residues and short-chain alkyl substituents. Moreover compounds 15, 16, and 17 had no immunosuppressive activity, which suggested that cis-3,4-dichlorinated proline played an important role in the immunosuppressive activity of Astin C.

Minimising conformational bias in fluoroprolines through vicinal difluorination

Monofluorination at the proline 4-position results in conformational effects, which is exploited for a range of applications. However, this conformational distortion is a hindrance when the natural proline conformation is important. Here we introduce (3S,

CARBOCYCLIC PROLINAMIDE DERIVATIVES

This invention is directed to novel carbocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk

SULFUR COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.