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Chirality holds the key for potent inhibition of the botulinum neurotoxin serotype a protease.

G Neil GN Stowe, Peter P Silhár, Mark S MS Hixon, Nicholas R NR Silvaggi, Karen N KN Allen, Scott T ST Moe, Alan R AR Jacobson, Joseph T JT Barbieri, and Kim D KD Janda

Org Lett 12(4):756-9 (2010) PMID 20092262

Botulinum neurotoxin serotype A (BoNT/A) is the most toxic protein known to man and also a bioterrorism agent. As defined by our previous research targeting the etiological agent responsible for BoNT/A intoxication, a protease, we now report on the asymmetric synthesis of four new BoNT/A inhibitors; the most potent of this series is roughly 2-fold more active than the best small molecule inhibitor currently known.

DOI: 10.1021/ol902820z
Version: za2963e q8zae q8zba q8zcf q8zde q8ze4 q8zf5 q8zgd
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