Application of 70-23-5

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Antimicrobial Chemotherapy called Repurposing ethyl bromopyruvate as a broad-spectrum antibacterial, Author is Kumar, Ajay; Boradia, Vishant Mahendra; Thakare, Ritesh; Singh, Alok Kumar; Gani, Zahid; Das, Swetarka; Patidar, Anil; Dasgupta, Arunava; Chopra, Sidharth; Raje, Manoj; Raje, Chaaya Iyengar, which mentions a compound: 70-23-5, SMILESS is O=C(OCC)C(CBr)=O, Molecular C5H7BrO3, Synthetic Route of C5H7BrO3.

Background: The emergence of drug-resistant bacteria is a major hurdle for effective treatment of infections caused by Mycobacterium tuberculosis and ESKAPE pathogens. In comparison with conventional drug discovery, drug repurposing offers an effective yet rapid approach to identifying novel antibiotics. Methods: Et bromopyruvate was evaluated for its ability to inhibit M. tuberculosis and ESKAPE pathogens using growth inhibition assays. The selectivity index of Et bromopyruvate was determined, followed by time-kill kinetics against M. tuberculosis and Staphylococcus aureus. We first tested its ability to synergize with approved drugs and then tested its ability to decimate bacterial biofilm. Intracellular killing of M. tuberculosis was determined and in vivo potential was determined in a neutropenic murine model of S. aureus infection. Results: We identified Et bromopyruvate as an equipotent broad-spectrum antibacterial agent targeting drug-susceptible and -resistant M. tuberculosis and ESKAPE pathogens. Et bromopyruvate exhibited concentration-dependent bactericidal activity. In M. tuberculosis, Et bromopyruvate inhibited GAPDH with a concomitant reduction in ATP levels and transferrin-mediated iron uptake. Apart from GAPDH, this compound inhibited pyruvate kinase, isocitrate lyase and malate synthase to varying extents. Et bromopyruvate did not neg. interact with any drug and significantly reduced biofilm at a 64-fold lower concentration than vancomycin. When tested in an S. aureus neutropenic thigh infection model, Et bromopyruvate exhibited efficacy equal to that of vancomycin in reducing bacterial counts in thigh, and at 1/25th of the dosage. Conclusions: Et bromopyruvate exhibits all the characteristics required to be positioned as a potential broad-spectrum antibacterial agent.

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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem