Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 13, 2006, Pages 3434-3439

  Palmer, James T ^a   Rydzewski, Robert M ^a   Mendonca, Rohan V ^a   Sperandio, David ^a   Spencer, Jeffrey R ^a   Hirschbein, Bernard L ^a   Lohman, Julia ^a   Beltman, Jeri ^a   Nguyen, Margaret ^a   Liu, Liang ^a  

^a CELERA   (United States)

Author keywords

Heterocycle; Inhibitor; Ketoheterocycle; Pharmacokinetics; Scaleable process; Selective; Serine protease; Tryptase

Indexed keywords

AMIDE; AROMATIC AMIDE; CARBAMIC ACID; CHYMASE; CHYMOTRYPSIN; ELASTASE; GRANZYME K; KALLIKREIN; PLASMIN; SERINE PROTEINASE; THROMBIN; TRYPSIN; TRYPTASE; TRYPTASE INHIBITOR; UNCLASSIFIED DRUG; UREA; UROKINASE;

ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG HALF LIFE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; HUMAN CELL; MAST CELL;

ANIMALS; BINDING SITES; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; HAPLORHINI; HUMANS; MAST CELLS; MICE; MOLECULAR STRUCTURE; OXADIAZOLES; SERINE ENDOPEPTIDASES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPTASES;

EID: 33646851222     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.04.013     Document Type: Article

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17. m (25 μM). The change in absorbance as a function of time was monitored at 405 nm.
18. iv,jv.