Desroy, Nicolas published the artcileNovel HldE-K Inhibitors Leading to Attenuated Gram Negative Bacterial Virulence, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2013), 56(4), 1418-1430, database is CAplus and MEDLINE.
The optimization of an HldE kinase inhibitor to low nanomolar potency is reported here, which resulted in the identification of the first reported compounds active on selected Escherichia coli strains. One of the most interesting candidates, compound 86, was shown to inhibit specifically bacterial LPS heptosylation on efflux pump deleted E. coli strains. This compound did not interfere with E. coli bacterial growth (MIC > 32 μg/mL) but sensitized this pathogen to hydrophobic antibiotics like macrolides normally inactive on Gram-neg. bacteria. In addition, 86 could sensitize E. coli to serum complement killing. These results demonstrate that HldE kinase is a suitable target for drug discovery. They also pave the way toward novel possibilities of treating or preventing bloodstream infections caused by pathogenic Gram-neg. bacteria by inhibiting specific virulence factors.
Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid.
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https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics