4-isobenzazole diketone containing small-molecule inhibitor and application in restraining ornithine decarboxylase (ODC)

Abstract

The invention provides a 4-isobenzazole diketone containing small-molecule inhibitor. The small-molecule inhibitor is 2-(2-4-prohexadione-1,2,3,4-tetralin-5-pyrimidyl)-5-{4-nitrophenoxyl}-1-H 4-isobenzazole-1,3(2H)-diketone, and the structural formula is shown in the specification. The 4-isobenzazole diketone containing small-molecule inhibitor is applied in restraining ornithine decarboxylase (ODC), preparing tumor treatment drugs and preparing pathogenic microorganism infection drugs, and a remarkable effect is achieved.

Description

technical field [0001] The invention relates to a small-molecule inhibitor of ornithine decarboxylase (Ornithine decarboxylase; ODC) and its application, in particular to a small-molecule inhibitor of human ornithine decarboxylase and its application in inhibiting and killing tumor cells. Background technique [0002] Protein is one of the main components of organisms and the main substance to complete various life activities. Among various proteins, proteases are crucial to life activities, and almost all biochemical reactions in organisms are catalyzed by proteases. The activity of various proteases in organisms has a strict regulation mechanism. Once there is a problem with the regulation mechanism, the activity of proteases is too high, too low or completely inactivated, which will cause various diseases. Therefore, it has very important theoretical and practical significance to regulate the activity of protease by drugs to restore and maintain it at a normal level. St...

AI Technical Summary

Problems solved by technology

However, its binding ability to ODC is weak, and its concentration is very high, and because it is a suicide inhibitor that forms a covalent bond with ODC, its toxic and side effects are very large

Images