Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377150 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
Abstract
Botulinum neurotoxins are the most toxic proteins currently known. Based on a recently identified potent lead structure, 2,4-dichlorocinnamic acid hydroxamate, herein we report on the structure–activity relationship of a series of hydroxamate BoNT/A inhibitors. Among them, 2-bromo-4-chlorocinnamic acid hydroxamate, 2-methyl-4-chlorocinnamic acid hydroxamate, and 2-trifluoromethyl-4-chlorocinnamic acid hydroxamate displayed comparable inhibitory activity to that of the lead structure.
Graphical abstractThe synthesis and SAR of a series of novel hydroxamate BoNT/A inhibitors is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kateřina Čapková, Yoshiyuki Yoneda, Tobin J. Dickerson, Kim D. Janda,