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Derivatives, preparation methods and uses of naftifine hydrochloride
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A drug, naphthyl technology, applied in the field of preparation of naftifine hydrochloride and its derivatives, can solve the problems of increasing bacterial resistance and increasing bacterial virulence
Active Publication Date: 2016-10-05
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI +1
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There are also some research reports that the golden yellow pigment can increase the resistance of bacteria to oleic acid. In the mouse subcutaneous infection model experiment, the abscess area caused by the mutant strain that cannot produce pigment is significantly smaller than that of the wild-type strain, suggesting that the pigment can increase the resistance of bacteria to oleic acid. Antioxidant ability to increase bacterial virulence
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[0121] The preparation method of the compound of formula I of the present invention or its pharmaceutically acceptable salt, comprises the following steps:
[0122]
[0123] (a) compound of formula II reacts with compound of formula III to generate compound of formula I; and optionally
[0124]
[0125] (b) the step of generating the hydrochloride salt of the compound of formula I from the compound of formula I,
[0126] In each formula, Ar is a C6-C10 aryl group, a C6-C10 aryl group substituted by a C1-C6 alkyl group.
[0127] In another preferred example, Ar is phenyl, naphthyl, or phenyl substituted by C1-C6 alkyl.
[0128] In another preferred embodiment, Ar is Among them, R 1 , R 2 independently C1-C6 alkyl or hydrogen; or R 1 , R 2 Together with adjacent carbon atoms, they form a C6-C10 aryl group.
[0129] In another preferred example, R 1 is hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl or tert-butyl, R 2 for hydrogen.
[0177] Example 2 Preparation of (E)-3-(4-methylphenyl)-prop-2-en-1-ol (intermediate IV-1).
[0178]
[0179] 100 mg of (E)-3-(4-methylphenyl)-acrolein was dissolved in 10 ml of methanol, and 26 mg of sodiumborohydride was added in batches under ice cooling, and reacted at room temperature for 15 minutes. After concentration, water was added to the residue, extracted three times with ethyl acetate, washed with saturated brine, dried over anhydrousmagnesiumsulfate, filtered, and concentrated to obtain 99 mg of the title compound as an oil, with a yield of 98%. Directly cast the next reaction.
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Abstract
The invention discloses a derivative, a preparation method and an application of naftifine hydrochloride. The derivative of naftifine hydrochloride of the present invention has a structure as shown in formula I. The present invention finds that by inhibiting the expression and / or function of the key catalytic enzyme CrtN in the aureus pigment synthesis pathway, the synthesis of aureus pigment can be strongly inhibited, thereby reducing the pathogenicity of bacteria. The key catalytic enzyme CrtN in the golden yellow pigment synthesis pathway can be used as a drug target, and compounds capable of inhibiting the expression and / or function of the catalytic enzyme CrtN can be used to prepare antibacterial drugs. Naftifine hydrochloride and its derivatives of the present invention can be used as inhibitors of catalytic enzyme CrtN, which can effectively inhibit the synthesis of golden yellow pigment, thereby reducing the pathogenicity of Staphylococcus aureus, and can be used to prepare antibacterial drugs, especially Preparation of drugs against Staphylococcus aureus infection.
Description
technical field [0001] The invention relates to the fields of pharmacology, medicinal chemistry and drug therapeutics, and more specifically relates to naftifine hydrochloride and its derivatives, a preparation method, a new antibacterial application, and a target CrtN for exerting an antibacterial effect. Background technique [0002] Staphylococcus aureus is an important pathogen that seriously endangers human life and health. As a representative of Gram-positive bacteria, it is the most common pathogen causing suppurative infection in humans, which can directly lead to local suppurative infection, pneumonia, pseudomembranous enteritis, pericarditis, etc., and even systemic infection such as sepsis and sepsis. [0003] With the development of life science and medicine, it has been found that pathogenic bacteria, including Staphylococcus aureus, are pathogenic because they produce various virulence factors (Virulence factors) to help bacteria colonize, adhere, cytotoxicity,...
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