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Fungal bis-Naphthopyrones as Inhibitors of Botulinum Neurotoxin Serotype A

  作者 CARDELLINA JOHN H II; ROXASDUNCAN VIRGINIA I; MONTGOMERY VICKI; ECCARD VANESSA; CAMPBELL YVETTE; HU XIN; KHAVRUTSKII ILJA; TAWA GREGORY J; WALLQVIST ANDERS; GLOER JAMES B; PHATAK NISARGA L; HOELLER ULRICH; SOMAN ASHISH G; JOSHI BIREN K; HEIN SARA M; WICKLOW DONALD T; SMITH LEONARD A  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2012年3-5;  页码  387-391  
  关联知识点  
 

[摘要]An in silico screen of the NIH Molecular Library Small Molecule Repository (MLSMR) of similar to 350000 compounds and confirmatory bioassays led to identification of chaetochromin A (1) as an inhibitor of botulinum neurotoxin serotype A (BoNT A). Subsequent acquisition and testing of analogues of 1 uncovered two compounds, talaroderxines A (2) and B (3), with improved activity. These are the first fungal metabolites reported to exhibit BoNT/A inhibitory activity.

 
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