Benkovic, Stephen J., Baker, Stephen J., Alley, M.R.K., Woo, Youn-Hi, Zhang, Yong-Kang, Akama, Tsutomu, Mao, Weimin, Baboval, Justin, Rajagopalan, P.T. Ravi, Wall, Mark, Kahng, Lyn Sue, Tavassoli, Ali and Shapiro, Lucy
Identification of borinic esters as inhibitors of bacterial cell growth and bacterial methyltransferases, CcrM and MenH
Journal of Medicinal Chemistry, 48, (23), . (doi:10.1021/jm050676a).
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As bacteria continue to develop resistance toward current antibiotics, we find ourselves in a continual battle to identify new antibacterial agents and targets. We report herein a class of boron-containing compounds termed borinic esters that have broad spectrum antibacterial activity with minimum inhibitory concentrations (MIC) in the low microgram/mL range. These compounds were identified by screening for inhibitors against Caulobacter crescentus CcrM, an essential DNA methyltransferase from gram negative alpha-proteobacteria. In addition, we demonstrate that borinic esters inhibit menaquinone methyltransferase in gram positive bacteria using a new biochemical assay for MenH from Bacillus subtilis. Our data demonstrate the potential for further development of borinic esters as antibacterial agents as well as leads to explore more specific inhibitors against two essential bacterial enzymes.
|Digital Object Identifier (DOI):
||anti-bacterial agents, chemical synthesis/chemistry/pharmacology
bacillus subtilis/drug effects/enzymology
borinic acids, chemical synthesis/chemistry/pharmacology
caulobacter crescentus/drug effects/enzymology
dna modification methylases, antagonists & inhibitors/chemistry
gram-negative bacteria, drug effects/enzymology/growth & development
gram-positive bacteria, drug effects/enzymology/growth & development
microbial sensitivity tests
||20 Mar 2007
||16 Apr 2017 18:42
|Further Information:||Google Scholar|
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