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.

Cregge, R J; Durham, S L; Farr, R A; Gallion, S L; Hare, C M; Hoffman, R V; Janusz, M J; Kim, H O; Koehl, J R; Mehdi, S; Metz, W A; Peet, N P; Pelton, J T; Schreuder, H A; Sunder, S; Tardif, C

Cregge, R J; Durham, S L; Farr, R A; Gallion, S L; Hare, C M; Hoffman, R V; Janusz, M J; Kim, H O; Koehl, J R; Mehdi, S; Metz, W A; Peet, N P; Pelton, J T; Schreuder, H A; Sunder, S; Tardif, C.

Affiliation

Cregge RJ; Hoechst Marion Roussel Inc., 2110 East Galbraith Road, Cincinnati, Ohio 45215, USA.

J Med Chem ; 41(14): 2461-80, 1998 Jul 02.

Article in En | MEDLINE | ID: mdl-9651152

Subject(s)

Drug Design; Ketones; Leukocyte Elastase/antagonists & inhibitors; Neutrophils/enzymology; Oligopeptides; Serine Proteinase Inhibitors; Administration, Oral; Animals; Azetidines/chemistry; Binding Sites; Cricetinae; Crystallography, X-Ray; Fluorocarbons/chemistry; Fluorocarbons/metabolism; Fluorocarbons/pharmacology; Hemorrhage/chemically induced; Hemorrhage/enzymology; Hemorrhage/prevention & control; Humans; Isoquinolines/chemistry; Ketones/chemical synthesis; Ketones/chemistry; Ketones/metabolism; Ketones/pharmacology; Leukocyte Elastase/metabolism; Lung Diseases/chemically induced; Lung Diseases/enzymology; Lung Diseases/prevention & control; Models, Molecular; Molecular Conformation; Oligopeptides/chemical synthesis; Oligopeptides/chemistry; Oligopeptides/metabolism; Oligopeptides/pharmacology; Pancreatic Elastase/antagonists & inhibitors; Pancreatic Elastase/metabolism; Proline/analogs & derivatives; Proline/chemistry; Serine Proteinase Inhibitors/chemical synthesis; Serine Proteinase Inhibitors/chemistry; Serine Proteinase Inhibitors/metabolism; Serine Proteinase Inhibitors/pharmacology; Structure-Activity Relationship; Swine

Search on Google

XML

PubMed Links

Collection: 01-internacional Database: MEDLINE Main subject: Oligopeptides / Drug Design / Serine Proteinase Inhibitors / Leukocyte Elastase / Ketones / Neutrophils Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 1998 Type: Article Affiliation country: United States

Search on Google

XML

PubMed Links