Analog of mono carbonyl structure of curcumin, and usage

Abstract

This invention relates to curcumin analogs and their applications. Curcumin is an excellent precursor compound, and has multiple pharmaceutical activities. The curcumin analogs in this invention have more stable monocarbonyl intermediate connection chain structure. The connection chain can be acetone, cyclopentanone or cyclohexanone. The substituent on benzene ring can be separately selected from H, hydroxyl, halogen, alkoxyl, alkyl, halogenated alkyl, amino, and alkyl amino. This invention also discloses pharmaceutically acceptable salts of the curcumin analogs, preparations containing them, and their pharmaceutical applications. Experiments show that the curcumin analogs can be used to treat inflammation and tumor.

Description

1. Technical field [0001] The present invention relates to a class of structural analogues of curcumin. Compared with curcumin, the structure of this type of compound only contains a carbonyl group; the present invention also relates to the preparation of such compounds, pharmaceutical preparations and their anti-inflammatory, anti-tumor aspects of use. 2. Background technology [0002] Curcumin is an important active ingredient found in almost all ginger plants. In India, Brazil, the Philippines, Japan, South Korea and other places, there are thousands of years of edible and medicinal records. Curcumin is a compound with strong pharmacological activity and wide indications. In recent years, medicinal chemistry and pharmacology studies have found that curcumin has various pharmacological effects such as anti-inflammation, anti-tumor, anti-angiogenesis, anti-mutation, anti-bacterial, anti-virus, anti-oxidation and neuroprotection. Curcumin has entered phase I in the United ...

AI Technical Summary

Problems solved by technology

[0018] Through a large number of documents and patents, we found that although it is generally believed that the active groups in the structure of curcumin are its phenolic hydroxyl group and β-diketone group, in curcumin analogues that do not contain these two active groups In terms of research, it has also been found that monocarbonyl curcumin analogues that do not contain β-diketones sometimes show stronger activity, which raises doubts that the β-diketone group is an essential group for the activity of curcumin

Moreover, due to the existence of the β-diketone structure, the stability of curcumin is weak, and it has better stability only when PH<6.5

[0019] It can be seen that the structure-activity relationship of curcumin may not be as simple as the current research, and drug screening using curcumin as a lead should not be completely based on the premise of retaining the phenolic hydroxyl group and diketone structure

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