1.
Bioorg Med Chem Lett
; 8(17): 2321-6, 1998 Sep 08.
Article
in English
| MEDLINE
| ID: mdl-9873535
ABSTRACT
The general approach of using a bicyclic template to produce inhibitors of the protease superfamily of enzymes has been investigated. The Diels Alder cycloaddition reaction on solid support has been found to be highly efficient for the synthesis of libraries of compounds that mimic the beta-strand secondary structure of proteins. Several potent and selective inhibitors of proteases have been discovered.
Subject(s)
Bridged Bicyclo Compounds, Heterocyclic/chemical synthesis , Peptide Library , Protease Inhibitors/chemical synthesis , Protein Structure, Secondary , Bridged Bicyclo Compounds, Heterocyclic/chemistry , Bridged Bicyclo Compounds, Heterocyclic/pharmacology , Chymases , Indicators and Reagents , Kallikreins/antagonists & inhibitors , Kinetics , Models, Molecular , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology , Serine Endopeptidases/metabolism , Serine Proteinase Inhibitors/chemical synthesis , Serine Proteinase Inhibitors/chemistry , Serine Proteinase Inhibitors/pharmacology , Structure-Activity Relationship , Thrombin/antagonists & inhibitors , Trypsin Inhibitors/chemical synthesis , Trypsin Inhibitors/chemistry , Trypsin Inhibitors/pharmacology , Tryptases
2.
J Chem Phys
; 50(8): 3606-10, 1969 Apr 15.
Article
in English
| MEDLINE
| ID: mdl-4306292