Fascaplysin derivative, preparation method and application of Fascaplysin derivative in MRSA (Methicillin Resistant Staphylococcus Aureus) resistance

A technology of derivatives and reactions, applied in antibacterial drugs, organic chemistry, etc., to achieve the effect of convenient and fast synthesis methods

Pending Publication Date: 2022-04-01
NINGBO UNIV
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However, the coupling reaction occurs selectively at the non-activated site...

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  • Fascaplysin derivative, preparation method and application of Fascaplysin derivative in MRSA (Methicillin Resistant Staphylococcus Aureus) resistance
  • Fascaplysin derivative, preparation method and application of Fascaplysin derivative in MRSA (Methicillin Resistant Staphylococcus Aureus) resistance
  • Fascaplysin derivative, preparation method and application of Fascaplysin derivative in MRSA (Methicillin Resistant Staphylococcus Aureus) resistance

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[0048] The present invention will be further described in detail below with reference to the accompanying drawings.

[0049] In the following embodiments, the same or similar reference numerals are initially, the same or similar original, or the original, as described below, and the embodiments described below are exemplary, only to explain the present invention, and cannot be understood In order to limit the invention.

[0050] The experimental test of the present application and the description of the drawings are as follows.

[0051] The FascaplySin derivative in this application is prepared by the following methods. (1) Put the raw material substrate dual halide β-pyramine compound (6-bromo-9H-pyridine [3,4-B] indole-1-yl) (2-chlorophenyl) meandenophenone, organic boric acid and The base is weighed in a certain molar ratio, and under an inert gas protection, a certain proportion of catalyst is added, and finally the reaction solvent is added, and the stirring is heated for a c...

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Abstract

The invention discloses a method for rapidly preparing a Fascaplysin derivative through a Suzuki-Miyaura coupling reaction and an application of the Fascaplysin derivative in resisting methicillin-resistant staphylococcus aureus (MRSA ATCC43300), and particularly discloses a method for rapidly preparing the Fascaplysin derivative through the Suzuki-Miyaura coupling reaction. The preparation method comprises the following steps: (1) carrying out regioselective Suzuki-Miyaura coupling on phenylboronic acid or heterocyclic boronic acid with different substituent groups and a dihalo-substituted raw material substrate, so as to obtain a series of Fascaplysin derivative precursor compound beta-carboline; and (2) carrying out intramolecular ring closing reaction on beta-carboline through high-temperature reaction, so as to obtain a series of Fascaplysin derivatives. According to the preparation method disclosed by the invention, a Fascaplysin derivative compound library with structural diversity can be quickly and efficiently constructed, and compared with the traditional Fascaplysin derivative synthesis, the preparation time is greatly shortened, and the synthesis efficiency is improved. The synthesized Fascaplysin derivative shows strong antibacterial activity, inhibits the formation of a biological membrane, and is an antibacterial drug candidate compound with a good application prospect.

Description

Technical field [0001] The present invention belongs to the chemical synthesis, the pharmaceutical field, in particular to the FascaplySin derivative precursor and FascaplySin derivative, and the present invention also relates to the rapid preparation method of these FascapLysin derivatives and its antimicrobial bacteria (MRSA) Application in. Background technique [0002] The wide use of antibiotics protects human health. However, excessive use and abuse of antibiotics also lead to rapid evolution of microbes, drug resistance and epidemic. According to the World Health Organization (WHO), it will be more than 10 million due to drug resistance due to drug resistance in 2050. Developed new antibiotics. Methylene Western Golden Staphylococcus aureus (MRSA) is one of the five most important pathogens that have been urgently needed to develop new antibiotics. The marine natural product has become an important source of pharmaceutical development in pharmaceutical development due to t...

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Application Information

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IPC IPC(8): C07D471/14A61P31/04
Inventor 蒋银丽梁洪泽裘弘达梁炜达赵星林嘉宇林俊浩刘莞王潇李咏梅赵玲玲
Owner NINGBO UNIV
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