Vinyl Sulfone Containing Parasitic Cysteinyl Protease Inhibitors

Title: Vinyl Sulfone Containing Parasitic Cysteinyl Protease Inhibitors

Volume: 7 Issue: 4

Author(s): Elizabeth Dunny and Paul Evans

Affiliation:

Keywords: Cruzain, cysteine proteases, parasitic inhibiotrs, peptides, rhodesain, vinyl sulfones, therapeutics targets, drug targets, parasitic diseases, metalloproteases

Abstract: Cysteine proteases are important therapeutic targets for numerous disease states including arthritis, osteoporosis, African sleeping sickness and Chagas disease. They have been shown to be viable drug targets for parasitic diseases through in vitro and animal model studies. This review examines the development of vinyl sulfone containing cysteine protease inhibitors. Peptidyl vinyl sulfones are superior inhibitors as they comprise the reactive vinyl sulfone warhead in addition to the peptide backbone, which has complementarity with the enzyme active site. The design, synthesis and activity of these protease inhibitors are discussed. Additionally, different methods for the preparation of vinyl sulfones are presented.

Cite this article as:

Dunny Elizabeth and Evans Paul, Vinyl Sulfone Containing Parasitic Cysteinyl Protease Inhibitors, Current Bioactive Compounds 2011; 7 (4) . https://dx.doi.org/10.2174/157340711798375859