Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors

…, R Pai, SC Cardinale, MM Butler, NP Peet…

Index: Li, Bing; Pai, Ramdas; Cardinale, Steven C.; Butler, Michelle M.; Peet, Norton P.; Moir, Donald T.; Bavari, Sina; Bowlin, Terry L. Journal of Medicinal Chemistry, 2010 , vol. 53, # 5 p. 2264 - 2276

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Citation Number: 31

Abstract

NSC 240898 was previously identified as a botulinum neurotoxin A light chain (BoNT/A LC) endopeptidase inhibitor by screening the National Cancer Institute Open Repository diversity set. Two types of analogues have been synthesized and shown to inhibit BoNT/A LC in a FRET-based enzyme assay, with confirmation in an HPLC-based assay. These two series of compounds have also been evaluated for inhibition of anthrax lethal factor (LF), ...