(3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative as well as preparation method and application thereof

A technology of phosphoric acid and derivatives, which is applied in the field of phenyl) phosphoric acid derivatives and their preparation, can solve problems such as insufficient bacterial resistance, and achieve excellent antibacterial activity and broad-spectrum inhibitory activity

Active Publication Date: 2021-08-06
SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the above-mentioned SBL inhibitors are ineffective against MBLs-regulated drug-resistant strains, so people continue to develop MBL inhibitors in order to obtain drugs against MBLs-producing drug-resistant strains
Although studies in recent years have found many compounds with good inhibitory activity on SBL or MBL, so far there is no MBL inhibitor on the market, and the existing inhibitors are not enough to solve the problem of bacterial resistance
In addition, because the structures and catalytic mechanisms of MBL and SBL are different, and carbapenem-resistant strains expressing both MBL and SBL have only emerged and spread in recent years, few compounds that jointly inhibit MBL and SBL have been reported so far.

Method used

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  • (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative as well as preparation method and application thereof
  • (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative as well as preparation method and application thereof
  • (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative as well as preparation method and application thereof

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Embodiment Construction

[0050] The raw materials and equipment used in the specific embodiment of the present invention are all known products, obtained by purchasing commercially available products.

[0051] 1. the preparation method of intermediate compound IV, comprises the following steps:

[0052]

[0053] Step 1: Dissolve 2-bromo-5-nitrobenzaldehyde 1 (2g, 8.69mmol) in 30ml ethanol, add sodium borohydride (166, 4.36mmol) three times at room temperature, react for 20 minutes, and monitor with TCL The degree of progress of the reaction, after the complete reaction, add 10ml of water to quench, then add 10ml of dichloromethane, shake the separatory funnel up and down for 1 minute, let stand to separate layers, collect the lower organic phase, repeat this process three times, combine the organic phases, and dry After drying over sodium sulfate, the solvent was concentrated and removed to obtain a crude product, which was obtained by column chromatography as a light yellow solid compound II (2-br...

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Abstract

The invention relates to the technical field of medicinal chemistry, and discloses a (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative derivative as shown in a formula X which is described in the specification. The derivative has good and broad-spectrum inhibitory activity on MBL and / or SBL enzyme, and can be used for preparing an MBL and / or SBL inhibitor. In addition, the compound provided by the invention can reverse the drug resistance of bacteria to carbapenem antibiotics. The (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative disclosed by the invention has great potential in preparation of drugs for overcoming drug resistance of beta-lactam antibiotics (the carbapenem antibiotics).

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivatives and a preparation method and application thereof. Background technique [0002] β-lactam antibiotics refer to a large class of antibiotics that contain a four-atom lactam ring in their chemical structure, including the most commonly used clinical penicillins, cephalosporins, carbapenems, and cephamycins, thiomycetes Atypical β-lactam antibiotics such as steroids and monocyclic β-lactams. β-lactam antibiotics are small-molecule antibacterial drugs widely used in clinical practice. They interfere with the synthesis of bacterial cell walls by inhibiting the activity of penicillin-binding proteins (PBPs), thereby leading to the death of bacteria. However, the efficacy of β-lactams is decreasing due to the rapid evolution and spread of bacterial resistance. The efficacy of carbapenem antibiotics, which are used as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6518C07F9/6558A61P31/04
CPCC07F9/6518C07F9/65583A61P31/04
Inventor 李国菠丁浩胜颜宇航朱开容吴勇
Owner SICHUAN UNIV
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