(3-(1h-1,2,3-triazole)phenyl)phosphoric acid derivatives, 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: 2022-05-27
SICHUAN UNIV
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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 derivatives, preparation method and application thereof
  • (3-(1h-1,2,3-triazole)phenyl)phosphoric acid derivatives, preparation method and application thereof
  • (3-(1h-1,2,3-triazole)phenyl)phosphoric acid derivatives, preparation method and application thereof

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Embodiment Construction

[0050] The raw materials and equipment used in the specific embodiments of the present invention are all known products, which are 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 (2 g, 8.69 mmol) in 30 ml of ethanol, add sodium borohydride (166, 4.36 mmol) three times at room temperature, and react for 20 minutes, monitored by TCL The degree of progress of the reaction, after the complete reaction, add 10 ml of water to quench, add 10 ml of dichloromethane, shake the separatory funnel up and down for 1 minute, let stand for stratification, collect the lower organic phase, repeat this process three times, combine the organic phases, After drying with aqueous sodium sulfate, the crude product was obtained by concentration and removal of the solvent, and the column chromatography gave a pale yellow solid compoun...

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Abstract

The present invention relates to the technical field of medicinal chemistry, and discloses a (3-(1H-1,2,3-triazole)phenyl)phosphoric acid derivative represented by a formula X, which is effective for MBL and / or The SBL enzyme has good and broad-spectrum inhibitory activity and can be used to prepare inhibitors of MBL and / or SBL; moreover, the compound of the invention can reverse the resistance of bacteria to carbapenem antibiotics. The (3-(1H-1,2,3-triazole) phenyl) phosphoric acid derivatives of the present invention have a very large effect on the preparation of drugs for overcoming the drug resistance of β-lactam antibiotics (carbapenem antibiotics) potential.

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 containing a four-atom lactam ring in the chemical structure, including the most commonly used clinical penicillins, cephalosporins, carbapenems, as well as cephamycins, thiomyces Atypical β-lactam antibiotics such as β-lactams 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 bacterial death. However, due to the rapid evolution and spread of bacterial resistance, the efficacy of β-lactams is declining. The efficacy of carbapenems, the class of antibiotics used as ...

Claims

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Application Information

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Patent Type & Authority Patents(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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