SIRT5 protein inhibitor and application thereof

A compound and alkyl technology, applied in the field of medicine, can solve the problem of low SIRT5 inhibitory activity and achieve significant protein inhibitory activity and multiple selection possibilities

Active Publication Date: 2021-11-09
XIHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] As the role of SIRT5 in different diseases is gradually revealed, SIRT5 inhibitors have been reported in recent years. However, only a few peptide analogs of these inhibitors have shown good in vivo and in vitro activities, and few non-peptide small Molecular inhibitors are not highly active against SIRT5 and are non-specific inhibitors

Method used

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  • SIRT5 protein inhibitor and application thereof
  • SIRT5 protein inhibitor and application thereof
  • SIRT5 protein inhibitor and application thereof

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Embodiment Construction

[0058] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some, not all, embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention. Unless otherwise specified, the technical means used in the implementation examples are conventional means well known to those skilled in the art.

[0059] The raw materials and equipment used in the specific embodiment of the present invention are all known products, obtained by purchasing commercially available products.

[0060] 1. The present invention discloses a compound of formula (I) or its stereoisomer, tautomer or salt thereof,

[0061]

[0062] wh...

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Abstract

The invention discloses a novel SIRT5 protein inhibitor and application thereof, and belongs to the technical field of medicines. The novel SIRT5 protein inhibitor has a structure shown in the general formula in the specification, wherein X is selected from one of NH or O; R1 is selected from one of H, alkyl, cycloalkyl, phenyl, substituted phenyl, heteroaromatic ring and substituted heteroaromatic ring; R2 is selected from one or more of the groups shown in the specification; R3 is selected from one of H, alkyl, cycloalkyl, aryl and substituted aryl; and R4 is selected from one of H, alkyl, cycloalkyl, aryl and substituted aryl. The invention provides a novel skeleton compound, the compound has obvious SIRT5 protein inhibition activity, and more selection possibilities are provided for development and application of an SIRT5 small-molecule inhibitor.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a novel SIRT5 protein inhibitor and its application. Background technique [0002] Silent Information Regulator 2 (SIRT) is a kind of NAD-dependent coenzyme + Atypical histone deacetylases that remove the acyl group on histone or non-histone lysine ε-N, including seven members of SIRT1-SIRT7. SIRT family proteins all have a Zn 2+ binding domain, a Rossmann fold domain and a catalytic core domain (i.e. substrate and NAD + binding site). Compared with other members of the SIRT family, SIRT5 contains a larger lysine acyl-binding pocket and contains a specific structural feature of tyrosine (Tyr102) and arginine residues (Arg105) in the pocket. In addition to weak deacetylation activity, it also has significant acid acylation activities such as demalonylation, desuccinylation and deglutamylation, and its catalytic efficiency is about 1000 times that of deacetylation. A large nu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/48A61K31/505A61P35/00A61P35/02
CPCC07D239/48A61P35/00A61P35/02Y02P20/55
Inventor 杨羚羚钱珊王周玉杨智文刘静
Owner XIHUA UNIV
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