Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones

…, P Bey, JP Burkhart, TM Chen, SL Durham…

文献索引：Angelastro; Baugh; Bey; Burkhart; Chen; Durham; Hare; Huber; Janusz; Koehl; Marquart; Mehdi; Peet Journal of Medicinal Chemistry, 1994 , vol. 37, # 26 p. 4538 - 4553

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被引用次数: 63

摘要

Valylprolylvalyl 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-morpholinylcarbonyl) benzoyl as the protecting group, 7l (MDL 101,146), was studied in greater detail. Hydration and ...