Design and synthesis of new orally active inhibitors of human neutrophil elastase

To identify new orally active inhibitors, further modification of 1 (ONO-6818) was performed. Peptidic derivatives 4b, 4c and 4n showed more potent inhibitory activity than nonpeptidic derivatives 3a– c. As a result, a series of peptidic inhibitors, 4a– s and 5a– v, were discovered. Among these N-ar...

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