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4.
1.
1 Physical and chemical properties and uses
Chloramphenicol (CAP) is a broad-spectrum antibiotic produced by Zipper mold Venezuela.
It is the first compound with a nitrogen atom found in nature, and it is also the world's first antibiotic that is manufactured in large quantities entirely by synthetic methods.
The L-body structure has antibacterial activity
.
Chloramphenicol antibiotics (chloramphenicols, CAPs) are also called amido alcohol antibiotics (amphenicols), including chloramphenicol, thiamphenicol (Tiamphenicol, TAP), palm chloramphenicol and so on
Table 4-1 The chemical structure of chloramphenicol antibiotics
4.
1.
1.
1 Physical and chemical properties
CAP is white needle-like crystals with extremely bitter taste.
It is a neutral organic compound, slightly soluble in water, stable in aqueous solution, and heat resistant.
It is easily soluble in ethanol, ethylene glycol , propylene glycol and acetamide, but insoluble in vegetable oils
.
In order to reduce the toxicity of CAP to the hematopoietic system, increase water solubility and bioavailability, etc.
TAP is a derivative in which the nitro group (—NO 2 ) is replaced by a methylsulfone group (-CH 3 SO 2 ) in the chemical structure of CAP .
It is a colorless and odorless crystalline powder with a slightly bitter taste and a neutral substance.
It is thermally stable and hygroscopic.
The solubility in water at room temperature is 0.
5% to 1%, and the solubility in alcohol is about 5%.
Its stability and solubility are not affected by pH
.
Florfenicol (FF) is a monofluoro derivative of TAP.
4.
1.
1.
2 Purpose
The antibacterial mechanism of CAPs is mainly to interfere with the synthesis of bacterial proteins
.
They can bind to the 50S subunit and are effective on 70S ribosomes, but have no effect on 80S ribosomes, so as to achieve the selectivity of sterilization
CAP is a broad-spectrum antibiotic that can inhibit the synthesis of bacterial protein, but it is strong against gram-negative bacteria, such as Escherichia coli, Salmonella, typhoid bacillus, paratyphoid bacillus, dysentery bacillus, aerobic bacillus, pneumonia bacillus, pneumococcus, chain bacteria, staphylococcus, diphtheria bacillus, anthrax bacillus
.
It also has a certain inhibitory effect on various rickettsiae, protozoa and some viruses
The antibacterial spectrum and antibacterial activity of FF are slightly better than CAP and TAP.
It is effective against both Gram-positive and Gram-negative bacteria, especially Pasteurella multocida, Actinomyces pleuropneumoniae, Mycoplasma pneumoniae and Streptococcus.
.
The 50% inhibitory concentration (MIC50) and 90% inhibitory concentration (MIC90) of the pathogenic bacteria of bovine respiratory diseases are respectively: Pasteurella hemolyticus 0.
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