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Paper | Special issue | Vol 79, No. 1, 2009, pp.487-520
Published online, 16th September, 2008
DOI: 10.3987/COM-08-S(D)8
Synthesis and Biological Evaluation of Inhibitors of Botulinum Neurotoxin Metalloprotease

Chenbo Wang, Julia Widom, Filip Petronijevic, James C. Burnett, Jonathan E. Nuss, Sina Bavari, Rick Gussio, and Peter Wipf*

*Department of Chemistry, University of Pittsburgh, Pittsburgh, Pennsylvania, 15260, U.S.A.


Based on the lead therapeutic agent NSC 240898, a new series of heterocyclic inhibitors of the BoNT serotype A metalloprotease has been generated. Highlights of the synthetic sequences include Sonogashira couplings of polysubstituted building blocks and gold-catalyzed indole formations. Preliminary structure-activity relationship studies afford detailed insights into the steric and electrostatic properties of the pharmacophore of this molecular scaffold.