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

Journal of Medicinal Chemistry

Volumn 41, Issue 14, 1998, Pages 2461-2480

  Cregge, Robert J ^a   Durham, Sherrie L ^a   Farr, Robert A ^a   Gallion, Steven L ^a,b   Hare, C Michelle ^a   Hoffman, Robert V ^a,c   Janusz, Michael J ^a   Kim, Hwa Ok ^a,c   Koehl, Jack R ^a   Mehdi, Shujaath ^a   Metz, William A ^a   Peet, Norton P ^a   Pelton, John T ^a   Schreuder, Herman A ^a   Sunder, Shyam ^a   Tardif, Chantal ^a  

^a SANOFI   (France)

^b ARQULE INC   (United States)

^c NEW MEXICO STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

COLLAGEN; ELASTASE INHIBITOR; ELASTIN; FIBRONECTIN; KETONE; LAMININ; LEUKOCYTE ELASTASE INHIBITOR; PENTAFLUOROETHYLKETONE; PROTEOGLYCAN; UNCLASSIFIED DRUG;

ADULT RESPIRATORY DISTRESS SYNDROME; ARTICLE; CHRONIC BRONCHITIS; CYSTIC FIBROSIS; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; LUNG EMPHYSEMA; PHAGOCYTOSIS; RHEUMATOID ARTHRITIS; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ADMINISTRATION, ORAL; ANIMALS; AZETIDINES; BINDING SITES; CRICETINAE; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; FLUOROCARBONS; HEMORRHAGE; HUMANS; ISOQUINOLINES; KETONES; LEUKOCYTE ELASTASE; LUNG DISEASES; MODELS, MOLECULAR; MOLECULAR CONFORMATION; NEUTROPHILS; OLIGOPEPTIDES; PANCREATIC ELASTASE; PROLINE; SERINE PROTEINASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; SWINE;

EID: 15444357089     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm970812e     Document Type: Article

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