Anti-protist activity of 2-(4,5-dichloroimidazolyl-1)-5 nitropyridine

FIELD: chemistry.

SUBSTANCE: disclosed is use of 2-(4,5-dichloroimidazolyl-1)-5-nitropyridine as an anti-protist agent. Anti-protist activity of 2-(4,5-dichloroimidazolyl-1)-5-nitropyridine is equal to 15.6 mcg/ml for Colpoda steinii. The substance can also relate to moderately toxic medicinal drugs.

EFFECT: high anti-protist activity.

1 tbl

 

The invention relates to the field of medicine and agriculture, namely to chemotherapeutic remedies to treat diseases caused by protozoa.

Known derivatives of a number of benzene with protistotsydnoe properties, for example, the drug himcocid and others (howansky AU,Ilyushechkin P., Kirillov P. Coccidiosis of poultry. - Leningrad, "Agropromizdat". - 1990. - p.71-91).

Known derivatives of pyrimidine with anticoccidial activity, for example the drug Baycox (toltrazuril, ametherm, intralox oral) and others. Baycox chosen as a prototype (Liping A.V. and others, 2002).

However, to Protistology drugs, including Bicocca, quickly emerging resistant strains of the parasite that causes to develop new drugs.

The aim of the invention is the use of 2-(4,5-dichloroimidazole-1)-5-nitropyridine as protesting funds. This goal is achieved by the synthesis and the establishment of Protistology activity of 2-(4,5-dichloroimidazole-1)-5-nitropyridine, which appeared in experiments in vitro in 2-4 times more active on the model of Colpoda steinii than a known drug baycox.

An example embodiment of the invention.

Synthesis of 2-(4,5-dichloroimidazole-1)-5-nitropyridine 1 is carried out according to the scheme

Method of synthesis: SMEs g (0.1 mol) of 2-chloro-5-nitropyridine 2, 13.7 g (0.1 mol) of 4,5-dichloroimidazole 3, 27.6 g (0.2 mol) of powdered potassium and 80 ml of dimethylformamide intensively stirred for 4 hours at 50-550°C. the Reaction mixture is cooled to 20-25°C and poured into 200 ml of water. Stirred for 10 minutes, the precipitate is filtered off, washed with water 3×50 ml Output 22.0 (85%), TPL 116-118°C. an NMR Spectrum1N, b, ppm: 8.042-8.071, doublet; 8.34, singlet; 8.83-8.87, Quartet; 9.36-9.37, doublet. Found, %: C, 37.45; H, 1.33; N, 21.91. C8H4Cl2N4O2. Calculated, %: C, 37.09; H, 1.55; N, 21.63.

Example test Protistology activity.

Protistology activity was determined by the method described in the book: "Scientific support of innovative development of the domestic animal. - Materials of all-Russian scientific-practical conference. - Novocherkassk, 2011. - The wildebeest SCRIVI RAAS. - S.162-165. As the test culture used the three-day culture coolpad species of Colpoda steinii. In addition Bicocca Comparators were amprolium, metronidazole (trichopol), furazolidone, sulfadimetoksin, ciprofloxacin. The results are given in the table.

Table
Protectina activity of 2-(4,5-dichloroimidazole-1)-5-nitropyridine
Medication Consider the drug concentration, µg/ml
100050025012562,531.25the 15.60,780,39
2-(4,5-dichloro-imidazolyl-1)-5-nitropyridine+++++++--
Furazolidone---------
Sulfadimetoksin---------
Trichopol- --------
Ciprofloxacin--------
Baycox (toltrazuril)++++++---
The amprolium+++++----
Water------ ---

Legend: (+) - all elementary killed

(-) - simple living

These tables show that the minimum protectina the potency of the compound 2-(4,5-dichloroimidazole-1)-5-nitropyridine 15.6 μg/ml, which is 4 times higher than that of Bicocca and amprolium. Other drugs in the studied concentrations did not show Protistology activity. Thus, in comparative tests of the substance 2-(4,5-dichloroimidazole-1)-5-nitropyridine detected high protectina activity.

The toxic properties of 2-(4,5-dichloroimidazole-1)-5-nitropyridine:

When introduced into the stomach of laboratory rats of this compound dose 0.2 g/kg 0.3 g/kg and 0.35 g/kg did not cause acute toxicity. Pre-matter may be referred to srednetonnazhnymi medicines.

References

1. Zubenko A.A. Definition Protistology activity of new compounds in the series of nitrogen-containing heterocycles / Sec, Linfatico, Annodam and other // "Scientific support of innovative development of the domestic animal Materials of all-Russian scientific-practical conference wildebeest, SCRIVI - Novocherkassk. 2011. - S.162-165.

2. Howansky AU, Ilyushechkin P., P. Kirillov Coccidiosis of poultry. - Leningrad, "agroindustrial trade is Izdat". - 1990. - P.71-91.

3. Liping A. Sanin A., Zinchenko E.V. Veterinary Handbook, M., 2002. - S.

The use of 2-(4,5-dichloroimidazole-1)-5-nitropyridine formula 1

as protesting funds.



 

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