Inhibition of Human Neutrophil Elastase with Peptidyl Electrophilic Ketones. 2. Orally Active PG-Val-Pro-Val Pentafluoroethyl Ketones

Valylprolyvalyl pentafluoroethyl ketones with different N-protecting groups were evaluated in vitro and in vivo as inhibitors of human neutrophil elastase (HNE). Several of these compounds were found to be orally active in HNE-induced rat and hamster lung hemorrhage models. The compound with 4-(4-mo...

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Veröffentlicht in:	Journal of medicinal chemistry 1994-12, Vol.37 (26), p.4538-4553
Hauptverfasser:	Angelastro, Michael R, Baugh, Larry E, Bey, Philippe, Burkhart, Joseph P, Chen, Teng-Man, Durham, Sherrie L, Hare, C. Michelle, Huber, Edward W, Janusz, Michael J
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Amino Acid Sequence Animals Chromatography, High Pressure Liquid Cricetinae Hemorrhage - drug therapy Humans Ketones - analysis Ketones - chemical synthesis Ketones - pharmacology Leukocyte Elastase Molecular Sequence Data Pancreatic Elastase - antagonists & inhibitors Rats Structure-Activity Relationship
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