Hydrazine nitrile cathepsin inhibitors with different P<3> structures, and application thereof

A technology of cathepsins and inhibitors, applied in the field of design and synthesis of cathepsins inhibitors, can solve problems such as side effects, and achieve the effects of easy synthesis, convenient synthesis and simple structure
CN102731344AInactive Publication Date: 2012-10-17JILIN UNIV
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Patent Information

Authority / Receiving Office
CN Β· China
Current Assignee / Owner
JILIN UNIV
Publication Date
2012-10-17
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The invention which belongs to the field of the design and the synthesis of cathepsin (Cat for short) inhibitors concretely relates to novel and efficient hydrazine nitrile inhibitors with different P<3> structures directed to four Cats (K, B, L and S). The main structure of the hydrazine nitrile inhibitors in the invention is represented by a formula in the specification; and in the formula, R1 is isobutyl, and R2 is alkyl, aryl, or cycloalkyl. The peptidomimetic hydrazine nitrile inhibitors designed and synthesized in the invention have the advantages of relatively simple structure, and easy synthesis; and the design and the synthesis of the maternal structure provide great conveniences for the synthesis of subsequent end products. Synthesized compounds, which can effectively inhibit actives of the Cat K, the Cat B, the Cat S and the Cat L, have an inhibition constant to the Cat K and the Cat L being in a picomole concentration (10<-12>M) level; and the synthesized compounds, which have weak inhibition effects on the Cat B and the Cat S have an inhibition constant being in a nanomole concentration (10<-9>M) level.
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Description

technical field

[0001] The invention belongs to the field of design and synthesis of cathepsins inhibitors, in particular to four cathepsins (K, B, L and S) with different P 3 A new type of high-efficiency hydrazinonitrile inhibitor with a bit structure. Background technique

[0002] Cathepsins (Cats) are the main members of the cysteine ​​protease family, and 11 species have been found in the human body. They are a class of intracellular proteases that mainly exist in lysosomes. They are unstable in neutral solutions and have low activity. They are easily activated and exert their physiological functions only in weakly acidic environments. [1] . Cats in lysosomes generate their active forms by hydrolyzing and cutting off the precursor peptides of some zymogens or prohormones, or activate other proteolytic enzyme systems to make them function. In addition to the main function of degrading proteins, Cats are also considered to be closely related to many important diseases ...

Claims

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