718642-08-1Relevant academic research and scientific papers
Hydrolytically-Resistant Boron-Containing Therapeutics And Methods Of Use
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Page/Page column 56, (2008/06/13)
Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.
Compounds for the Treatment of Periodontal Disease
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Page/Page column 57, (2008/06/13)
Compounds, compositions and methods are provided which are useful in the treatment of periodontal disease.
Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), for the potential treatment of onychomycosis
Baker, Stephen J.,Zhang, Yong-Kang,Akama, Tsutomu,Lau, Agnes,Zhou, Huchen,Hernandez, Vincent,Mao, Weimin,Alley,Sanders, Virginia,Plattner, Jacob J.
, p. 4447 - 4450 (2007/10/03)
A structure-activity relationship investigation for a more efficacious therapy to treat onychomycosis, a fungal infection of the toe and fingernails, led to the discovery of a boron-containing small molecule, 5-fluoro-1,3-dihydro- 1-hydroxy-2,1-benzoxaborole (AN2690), which is currently in clinical trials for onychomycosis topical treatment.
Identification of borinic esters as inhibitors of bacterial cell growth and bacterial methyltransferases, CcrM and MenH
Benkovic, Stephen J.,Baker, Stephen J.,Alley,Woo, Youn-Hi,Zhang, Yong-Kang,Akama, Tsutomu,Mao, Weimin,Baboval, Justin,Rajagopalan, P. T. Ravi,Wall, Mark,Kahng, Lyn Sue,Tavassoli, Ali,Shapiro, Lucy
, p. 7468 - 7476 (2007/10/03)
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 α-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.
