The general approach of using a bicyclic template to produce inhibitor
s of the protease superfamily of enzymes has been investigated. The Di
els-Alder cycloaddition reaction on solid support has been found to be
highly efficient for the synthesis of libraries of compounds that mim
ic the beta-strand secondary structure of proteins. Several potent and
selective inhibitors of proteases have been discovered. (C) 1998 Else
vier Science Ltd. All rights reserved.