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Application of tetrahydroisoquinoline compound for preparing drug killing animal mites

A technology of tetrahydroisoquinoline and compound, applied in the direction of drug combination, organic chemistry, anti-infective drugs, etc., can solve the problems of bad, no reports, frequent recurrence and repeated infection, etc.

Active Publication Date: 2014-06-04
内蒙古恒光大药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present, abamectin class acaricides are facing serious problems in three aspects: one, like all chemical drugs, along with the long-term use of abamectin class drugs, more and more mites have produced With the increasingly serious drug resistance, the recurrence and superinfection of acariasis are becoming more and more frequent; secondly, the adverse environmental and ecological impacts caused by abamectins due to their broad-spectrum, high-efficiency, and stable characteristics have aroused strong concern. Residual drugs in animal excrement can seriously affect the decomposition process of many normal microorganisms and protozoa; third, abamectin drugs can only drive and kill insects, but are ineffective against eggs. Only repeated medication can improve the rate of deworming rate, prevent the recurrence of mite
However, there is no report about the application of these compounds as acaricides

Method used

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  • Application of tetrahydroisoquinoline compound for preparing drug killing animal mites
  • Application of tetrahydroisoquinoline compound for preparing drug killing animal mites
  • Application of tetrahydroisoquinoline compound for preparing drug killing animal mites

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Experimental program
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Embodiment Construction

[0018] Figure 1~3 Combined with in vitro acaricidal activity test description.

[0019] In the present invention, the applicant designed and synthesized a series of 1-cyano-2-aryl-1,2,3,4-tetrahydroisoquinoline compounds with the general structural formula as follows:

[0020]

[0021] Wherein, R is ortho, meta or para alkyl, alkoxy, halogen, hydroxyl, nitro, trifluoromethyl, cyano and the like.

[0022] The present invention is used to prepare the synthetic route of series 1-cyano-2-aryl-1,2,3,4-tetrahydroisoquinoline compounds as follows:

[0023]

[0024] The applicant has carried out pharmacological activity research on the above-mentioned compound by adopting an in vitro acaricidal activity test. In the in vitro acaricidal activity test, the acaricidal activity of each test compound at the same concentration was determined by the drug dipping method, and compared with the commonly used clinically used acaricidal drug - ivermectin. Mortality indicates the level o...

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PUM

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Abstract

The invention discloses application of a tetrahydroisoquinoline compound for preparing a drug killing animal mites. The compound has the molecular structure feature shown in the specification, wherein R is ortho-, meta- or para-alkyl, alkoxy, halogen, hydroxyl, nitro, trifluoromethyl, cyano group and the like. The compound has good activity in killing multiple animal mites like psoroptes communis cuniculi, which is superior to that of the clinical mite killing drug ivermectin, and has chemical stability and good compatibility with physiological environment.

Description

technical field [0001] The invention relates to the application of a class of tetrahydroisoquinoline compounds as animal acaricides. Background technique [0002] Livestock and poultry acariasis is a kind of ectoparasitic disease that is ubiquitous and seriously endangers the health of animals. It is characterized by contact infection, severe itching and severe skin inflammation. It can cause severe stress reactions in animals and affect animal feeding and sleep. , feed efficiency and animal weight gain, severe cases can cause animal death. The occurrence of animal mites is very common and quite stubborn. Pigs, sheep, cattle, chickens, rabbits, dogs, foxes, mice, etc. are all infected with mites and the incidence is very high. Therefore, the disease seriously affects the production performance of animals and the quality of livestock products. In addition, mites also play an intermediary role in the spread of bacterial and viral diseases. [0003] For a long time, the cont...

Claims

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Application Information

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IPC IPC(8): C07D217/26A61K31/472A61P33/14
CPCC07D217/26
Inventor 周乐
Owner 内蒙古恒光大药业股份有限公司
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