175012-20-1

Upstream product

• 66831-16-1 O-benzyl-trans-4-hydroxy-L-proline hydrochloride 
• 175012-19-8 (2S,4R)-4-Benzyloxy-1-((S)-2-tert-butoxycarbonylamino-3-methyl-butyryl)-pyrrolidine-2-carboxylic acid 
• 172089-25-7 4-(t-Butoxycarbonyl)amino-1,1,1,2,2-pentafluoro-5-methylhex-an-3-one 
• 40350-83-2 (2S,4R)-4-(benzyloxy)-1-(tert-butoxycarbonyl)pyrrolidine-2-carboxylic acid 
• 58561-04-9 N-tert-butoxycarbonyl-L-valine methyl ester 
• 13734-41-3 t-Boc-L-valine 
• 3392-12-9 Boc-Val-ONSu 

Relevant academic research and scientific papers

Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones

A series of P2-modified, orally active peptidic inhibitors of human neutrophil elastase (HNE) are reported. These pentafluoroethyl ketone-based inhibitors were designed using pentafluoroethyl ketone 1 as a model. Rational structural modifications were made at the P3, P2, and activating group (A(G)) portions of 1 based on structure-activity relationships (SAR) developed from in vitro (measured K(i)) data and information provided by modeling studies that docked inhibitor 1 into the active site of HNE. The modeling-based design was corroborated with X-ray crystallographic analysis of the complex between 1 and porcine pancreatic elastase (PPE) and subsequently the complex between 1 and HNE.