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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