Su, Jianpeng published the artcileEbsulfur as a potent scaffold for inhibition and labelling of New Delhi metallo-¦Â-lactamase-1 in vitro and in vivo, Synthetic Route of 119-80-2, the publication is Bioorganic Chemistry (2019), 192-201, database is CAplus and MEDLINE.
The superbug infection caused by New Delhi metallo-¦Â-lactamase (NDM-1) has grown into an emerging threat, labeling and inhibition of NDM-1 has proven challenging due to its shuttling between pathogenic bacteria. Here, we report a potent covalent scaffold, ebsulfur, for targeting the protein in vitro and in vivo. Enzymic kinetic study indicated that eighteen ebsulfurs gained except 1a-b and 1f inhibited NDM-1, exhibiting an IC50 value ranging of 0.16-9 ¦ÌM, and 1g was found to be the best, dose- and time-dependent inhibitor with an IC50 of 0.16 ¦ÌM. Also, these ebsulfurs effectively restored the antibacterial activity of cefazolin against E. coli expressing NDM-1, and the best effect was observed to be from 1g, 1i and 1n, resulting in an 256-fold reduction in MIC of the antibiotic at a dose of 16 ¦Ìg/mL. The equilibrium dialysis study implied that the ebsulfur disrupted the coordination of one Zn(II) ion at active site of NDM-1. Labeling of NDM-1 using a constructed fluorescent ebsulfur Ebs-R suggested that the inhibitor covalently bound to the target through SDS-PAGE anal. in vitro. Also, labeling NDM-1 in living E. coli cells with Ebs-R by confocal microscopic imaging showed the real-time distribution change process of intracellular recombinant protein NDM-1. Moreover, the cytotoxicity of these ebsulfurs against L929 mouse fibroblastic cells was tested, and their capability to restore antibacterial activity of antibiotic against clin. strains E. coli EC08 producing NDM-1 was determined The ebsulfur scaffold proposed here is valuable for development of the covalent irreversible inhibitors of NDM-1, and also for labeling the target in vitro and in vivo.
Bioorganic Chemistry published new progress about 119-80-2. 119-80-2 belongs to catalysis-chemistry, auxiliary class sulfides,Carboxylic acid,Benzene, name is 2,2′-Dithiodibenzoic acid, and the molecular formula is C8H10N2O2, Synthetic Route of 119-80-2.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia