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    Home > Chemicals Industry > Chemical Technology > The physical and chemical properties and uses of quinolones

    The physical and chemical properties and uses of quinolones

    • Last Update: 2021-09-19
    • Source: Internet
    • Author: User
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    11.
    1.
    1 Physical and chemical properties and uses

    Quinolones (quinolones, QNs), also known as pyridonic acids or pyridonic acids, are compounds with 1,4-dihydro-4-oxopyridine-3-carboxylic acid as the basic ring structure.
    They are derived from nalidixic acid or The basic structure of a synthetic antibacterial drug derived from pyridoxine is shown in Figure 11-1
    .

    In 1962, Lesher et al.
    discovered the first QNs-nalidixic acid, and through structural modification and modification of it, it enhanced its biological and pharmacological activities
    .


    A ring structure is required antibacterial effect, must Parallelism aromatic or heterocyclic ring and B ring may be major changes, may be a benzene ring, a pyridine ring, a pyrimidine ring or the like


    Figure 11-1 Basic structure of QNs

    The introduction of fluorine atoms at the C 6 position has become a significant feature of the FQs structure
    .


    Its ability to bind to DNA gyrase is increased by 2 to 17 times, which can enhance the inhibitory effect on DNA helicase; its antibacterial activity against gram-positive bacteria is enhanced, and its penetration into cells is increased by 1 to 70 times


    In 1997, Aandriole proposed to use the Aandriole-Schellhore classification method compiled by Schellhore to divide QNs into four generations.
    The international academic community also divided the development of QNs into four stages according to this method: the first generation of QNs, the main representative is nalidixic acid, Only effective against Escherichia coli, Shigella, Pneumoniae, Proteus and Salmonella, etc.
    : It has weak or ineffective effect on Gram-positive bacteria and Pseudomonas aeruginosa
    .


    Because of its poor curative effect and easy development of drug resistance, it has been seldom used clinically


    11.
    1.
    1.
    1 Physical and chemical properties

    QNs are all white or light yellow crystalline powders
    .


    Most of the melting points are above 200°C (melting is accompanied by decomposition), and the melting point can exceed 300°C after salt formation


    Table 11-1 Physical and chemical properties of commonly used QNs

     

     

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