2-amino-5-heteroaryl substituted pyrazine derivative and application thereof

Abstract

The invention provides a 2-amino-5-heteroaryl substituted pyrazine derivative with a chemical structure as shown in a formula 1, a pharmaceutical preparation containing the 2-amino-5-heteroaryl substituted pyrazine derivative, and application of the 2-amino-5-heteroaryl substituted pyrazine derivative in drugs for treating or preventing malaria. Compared with the prior art, the compound has the effects of resisting plasmodium falciparum proliferation and resisting plasmodium falciparum of different strains, and has the advantages of longer half-life period, lower plasma clearance rate, higher distribution volume and better oral bioavailability.

Description

technical field

[0001] The invention relates to a pyrazine derivative, in particular to a 2-amino-5-heteroaryl substituted pyrazine derivative and its application in medicines for preventing or treating malaria. Background technique

[0002] Malaria is a disease endemic in many developing countries. About 40% of the world's population lives in countries where the disease is endemic; approximately 247 million people suffer from the disease each year.

[0003] A variety of drugs, including combinations of drugs, are currently used to treat malaria, however, many of these drugs are expensive, and some exhibit significant toxicity and unwanted side effects in humans, and, drug-resistant malaria strains The emergence has become a significant problem in the current malaria treatment. WHO recommends artemisinin combined with other types of antimalarial drugs as the first-line treatment for malaria caused by P. The suspected emergence of artemisinin-resistant Plasmodium falciparum...

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