Peptide inhibitors of dengue virus NS3 protease. Part 1: Warhead

Substrate-based tetrapeptide inhibitors with various warheads were designed, synthesized, and evaluated against the Dengue virus NS3 protease. Effective inhibition was achieved by peptide inhibitors with electrophilic warheads such as aldehyde, trifluoromethyl ketone, and boronic acid. A boronic acid has the highest affinity, exhibiting a K-i of 43 nM. (c) 2005 Elsevier Ltd. All rights reserved.