328547-41-7Relevant articles and documents
Synthesis and biological evaluation of inhibitors of botulinum neurotoxin metalloprotease
Wang, Chenbo,Widom, Julia,Petronijevic, Filip,Burnett, James C.,Nuss, Jonathan E.,Bavari, Sina,Gussio, Rick,Wipf, Peter
experimental part, p. 487 - 520 (2009/12/24)
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.