Lee, Minhee published the artcileStructure-Activity Relationship of Sulfonyl Piperazine LpxH Inhibitors Analyzed by an LpxE-Coupled Malachite Green Assay, Recommanded Product: tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate, the publication is ACS Infectious Diseases (2019), 5(4), 641-651, database is CAplus and MEDLINE.
The UDP-2,3-diacylglucosamine pyrophosphatase LpxH in the Raetz pathway of lipid A biosynthesis is an essential enzyme in the vast majority of Gram-neg. pathogens and an excellent novel antibiotic target. The 32P-radioautog. thin-layer chromatog. assay has been widely used for anal. of LpxH activity, but it is inconvenient for evaluation of a large number of LpxH inhibitors over an extended time period. Here, we report a coupled, nonradioactive LpxH assay that utilizes the recently discovered Aquifex aeolicus lipid A 1-phosphatase LpxE for quant. removal of the 1-phosphate from lipid X, the product of the LpxH catalysis; the released inorganic phosphate is subsequently quantified by the colorimetric malachite green assay, allowing the monitoring of the LpxH catalysis. Using such a coupled enzymic assay, we report the biochem. characterization of a series of sulfonyl piperazine LpxH inhibitors. Our anal. establishes a preliminary structure-activity relationship for this class of compounds and reveals a pharmacophore of two aromatic rings, two hydrophobic groups, and one hydrogen-bond acceptor. We expect that our findings will facilitate the development of more effective LpxH inhibitors as potential antibacterial agents.
ACS Infectious Diseases published new progress about 945953-41-3. 945953-41-3 belongs to piperazines, auxiliary class Piperazine,Amide,Aldehyde, name is tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate, and the molecular formula is C11H20N2O3, Recommanded Product: tert-Butyl 4-(2-oxoethyl)piperazine-1-carboxylate.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics