Fungal bis-Naphthopyrones as Inhibitors of Botulinum Neurotoxin Serotype A
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- 作者：John H. Cardellina ; II ; Virginia I. Roxas-Duncan ; Vicki Montgomery ; Vanessa Eccard ; Yvette Campbell ; Xin Hu ; Ilja Khavrutskii ; Gregory J. Tawa ; Anders Wallqvist ; James B. Gloer ; Nisarga L. Phatak ; Ulrich H枚ller ; Ashish G. Soman ; Biren K. Joshi ; Sara M. Hein ; Donald T. Wicklow ; Leonard A. Smith
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：May 10, 2012
- 年：2012
- 卷：3
- 期：5
- 页码：387-391
- 全文大小：293K
- 年卷期：v.3,no.5(May 10, 2012)
- ISSN：1948-5875
文摘
An in silico screen of the NIH Molecular Library Small Molecule Repository (MLSMR) of 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.