Synthesis and Activity of Biomimetic Biofilm Disruptors
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Böttcher, Thomas
Kolodkin-Gal, Ilana
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https://doi.org/10.1021/ja3120955Metadata
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Böttcher, Thomas, Ilana Kolodkin-Gal, Roberto Kolter, Richard Losick, and Jon Clardy. 2013. Synthesis and activity of biomimetic biofilm disruptors. Journal of the American Chemical Society 135(8): 2927-2930.Abstract
Biofilms are often associated with human bacterial infections, and the natural tolerance of biofilms to antibiotics challenges treatment. Compounds with antibiofilm activity could become useful adjuncts to antibiotic therapy. We used norspermidine, a natural trigger for biofilm disassembly in the developmental cycle of Bacillus subtilis, to develop guanidine and biguanide compounds with up to 20-fold increased potency in preventing biofilm formation and breaking down existing biofilms. These compounds also were active against pathogenic Staphylococcus aureus. An integrated approach involving structure–activity relationships, protonation constants, and crystal structure data on a focused synthetic library revealed that precise spacing of positively charged groups and the total charge at physiological pH distinguish potent biofilm inhibitors.Other Sources
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3585461/pdf/Terms of Use
This article is made available under the terms and conditions applicable to Other Posted Material, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#LAACitable link to this page
http://nrs.harvard.edu/urn-3:HUL.InstRepos:10611830
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