Amide derivative and purpose thereof

Abstract

The invention relates to an amide derivative and a purpose thereof. The invention discloses an N-(4-substiguted aminoacyl phenyl)-5-substited furan-2-formamide compound and tests the activity of the compound for inhibiting falcipain-2 in experiment of enzyme level in vitro, and the result indicates that the compound has strong inhibitory activity to falcipain- 2. Therefore, the N-(4-substiguted aminoacyl phenyl)-5-substited furan-2-formamide compound provided in the invention can act as cysteine protease (falcipain-2) inhibitor in food vacuole of plasmodium to stop further proliferation of plasmodium in a host.

Description

technical field

[0001] The present invention relates to an amide derivative and its use, in particular to an N-(4-substituted aminoacylphenyl)-5-substituted furan-2-carboxamide compound and its use. Background technique

[0002] Malaria, the most frequent parasitic disease on Earth, is a potentially fatal disease transmitted by Anopheles mosquitoes. With the continuous increase of drug resistance to existing antimalarial drugs, the incidence of malaria is increasing, and the discovery of new antimalarial drugs with therapeutic effects is urgently needed.

[0003] Plasmodium in the erythrocytic stage hydrolyzes the host's hemoglobin in its acidic food vacuole to obtain the energy and amino acids needed for its own life. Biological studies have shown that the food vesicles of Plasmodium contain a series of hydrolytic enzymes, such as plasmepsins, falcipains, and falcilysins. These enzymes have emerged as potential targets for malaria chemotherapy.

[0004] Cysteine ​​protea...

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