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Application of Sulfaclozine and its derivatives

A technology of sulfachlorpyrazine and sulfachlorpyrazine sodium, which is applied in the field of medicine, can solve the problems of inability to completely kill parasites, large toxic and side effects, long medication time, etc., and achieves great application value and market prospects, drug safety, less toxic effect

Inactive Publication Date: 2010-11-24
SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the existing anti-toxoplasma drugs can not completely kill parasites, the relapse rate after drug withdrawal is high, and because these drugs take a long time, the side effects are relatively large, therefore, it is necessary to find a kind of high-efficiency, low toxicity Antitoxoplasma drugs

Method used

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  • Application of Sulfaclozine and its derivatives
  • Application of Sulfaclozine and its derivatives
  • Application of Sulfaclozine and its derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The preliminary screening test of embodiment 1 anti-toxoplasma gondii drug

[0017] In order to find effective anti-toxoplasma drugs, six drugs (azithromycin, tiamulin, clarithromycin, sulfachlorpyrazine sodium, metronidazole, and trimethoprim) that are commonly used in clinical practice were selected for anti-toxoplasma. Preliminary experiment of Toxoplasma gondii infection in mice.

[0018] (1) Preliminary experiment of comparison of 6 drugs

[0019] Set up 7 groups, 10 Kunming male mice in each group, 70 in total. Use the tachyzoites of Toxoplasma gondii (Toxoplasma gondii) Changning strain (CN strain, a virulent strain isolated from Shanghai diseased pigs), and press 1×10 4 Each mouse was intraperitoneally inoculated with mice, and the drug group was administered orally 4 hours after inoculation (see Table 1 for the drugs and doses used in each group), and the drug was used continuously for 6 days. On the 6th and 7th days after inoculation, each group was necropsi...

Embodiment 2

[0036] Embodiment 2 Different sulfonamide drug curative effect comparison experiment

[0037] Sulfonamides are a class of antibacterial drugs widely used in humans and animals. The mechanism of action of sulfa drugs is to interfere with the folic acid metabolism of Toxoplasma gondii, so that the growth and reproduction of Toxoplasma gondii are inhibited. Under normal conditions, Toxoplasma uses p-aminobenzoic acid to synthesize tetrahydrofolate with the participation of dihydrofolate synthase and reductase, and the basic structure of sulfonamides is similar to p-aminobenzoic acid, which can be combined with p-aminobenzoic acid Competing with each other for dihydrofolate synthase, hindering the formation of dihydrofolate so as to affect the synthesis of nucleic acid and protein, thereby inhibiting the growth and reproduction of Toxoplasma gondii. The compound of sulfadiazine and pyrimethamine is the control drug in the experiment of anti-toxoplasma gondii drug.

[0038] (1) E...

Embodiment 3

[0046] The drug safety test of embodiment 3 different sulfa drugs

[0047] Grouped healthy mice were directly fed with different drugs, and indicators such as health and body weight were observed. The mice were divided into 8 groups. The first 7 groups were fed with 7 different sulfa drugs for 5 days (see Table 5), and the 8th group was fed with the same amount of normal saline. During the experiment, each mouse was weighed every five days and the health status of the mice was recorded every day. The experiment lasted for 25 days.

[0048] The results showed that all the drugs were not lethal at the dose of 250mg / kg / day. The changes in body weight in Table 5 show that there is no significant difference between the weight gain of the trimethoprim lactate (TMP) irrigation group and the healthy control group. Sulfamethazine sodium (SDD), sulfamethoxypyridazine sodium (SMP) and sulfamethoxypyridazine sodium (SPZ) significantly increased the weight of mice compared with other dru...

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Abstract

The invention discloses an application of Sulfaclozine and its derivatives used for treating toxoplasmosis. The invention also discloses an anti-toxoplasmosis medicinal composition, containing an effective component sulfaclozine or derivatives thereof. The sulfaclozine and derivatives thereof have remarkable toxoplasmosis resistance, and are expected to become a new generation medicament for treating the toxoplasmosis.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the use of sulfachlorpyrazine and derivatives thereof. Background technique [0002] Toxoplasmosis is caused by Toxoplasma gondii (Toxoplasma gondii), a very widespread global zoonotic disease, which can be transmitted between humans and cattle, sheep, pigs, chickens and other animals. Toxoplasma gondii is an obligate intracellular parasitic protozoa belonging to the order Eucoccidia, Sarcocystinidae, which can infect almost all warm-blooded animals. After animals are infected with Toxoplasma gondii, on the one hand, their production performance is affected, and on the other hand, they become the source of infection of human toxoplasmosis. Therefore, the prevention and treatment of animal toxoplasmosis has important economic and public health significance. Humans are seriously infected with toxoplasmosis. According to the second national survey on important human parasitic dis...

Claims

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Application Information

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IPC IPC(8): A61K31/635A61P33/02
Inventor 黄兵王权曾艳波朱顺海韩红玉陈永军董辉姜连连蒋蔚赵其平程军马卫娇
Owner SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI