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Nitroimidiazoles are antiprotozoal drugs containing a nitro heterocyclic structure
.
In 1954, metronidazole was synthesized for the treatment of trichomoniasis, amoebiasis and Giardiasis: In 1962, it was discovered that metronidazole has a strong antibacterial effect on anaerobic bacteria.
16.
1.
1 Physical and chemical properties and uses
16.
1.
1.
1 Physical and chemical properties
Nitroimidazole drugs are white or light yellow crystals, which are easily decomposed when exposed to light, can be vaporized, and are easily volatile when dried for a long time; they are soluble in water, acetone , methanol , ethanol, chloroform and ethyl acetate to varying degrees ; most of them are weakly alkaline , Soluble in acid solution, combined with acid to form salt, unstable in alkaline solution
.
The physical and chemical properties of common nitroimidazole drugs and their metabolites are shown in Table 16-1
Table 16-1 Physical and chemical properties of common nitroimidazole drugs and their metabolites
16.
1.
Nitroimidazole drugs have antiprotozoal and antibacterial activities, and also have a strong anti-anaerobe effect
.
After the drug enters the susceptible microbial cells, the nitro group is reduced by the electron transfer protein to the amino group with cytotoxic effect under the anaerobic or low oxygen environment and low redox potential, thereby inhibiting the synthesis of cellular DNA and making The synthesized DNA is degraded, destroying the double helix structure of the DNA or blocking its transcription and replication, thereby causing cell death, exerting its role in rapidly killing anaerobic bacteria and effectively controlling infection
The biological activity of nitroimidazole drugs is closely related to its chemical structure, and 1-methyl-5-nitroimidazole is the biologically active group of such compounds
.
The antiprotozoal activity of drugs is related to the lipophilicity and electronegativity of the imidazole ring, and the antibacterial activity is related to electrolytic reduction
Nitroimidazole drugs are mainly used to treat protozoan infections, such as bovine trichomoniasis, canine giardiasis, chicken and turkey histotrichomoniasis, avian giardiasis, acute amoebic dysentery and parenteral amoeba Sick
.
In addition, it has the effect of resisting bee microsporidiosis and amoebiasis
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