Heterocycles

Synthesis and biological evaluation of inhibitors of botulinum neurotoxin metalloprotease

C Wang, J Widom, F Petronijevic, JC Burnett, JE Nuss…

Index: Wang, Chenbo; Widom, Julia; Petronijevic, Filip; Burnett, James C.; Nuss, Jonathan E.; Bavari, Sina; Gussio, Rick; Wipf, Peter Heterocycles, 2009 , vol. 79, # C p. 487 - 520

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Citation Number: 22

Abstract

Résumé/Abstract-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 ...