Nonpeptidic Inhibitors of Human Leukocyte Elastase. 3. Design, Synthesis, X-ray Crystallographic Analysis, and Structure-Activity Relationships for a Series of Orally Active 3-Amino-6-phenylpyridin-2-one Trifluoromethyl Ketones

Article abstract of DOI:10.1021/jm00046a016

A series of nonpeptidic inhibitors of human leukocyte elastase (HLE) is reported.These trifluoromethyl ketone-based inhibitors contain a 3-amino-6-phenylpyridone group as a central template.The effect of varying the N-3 substituent in these inhibitors on