KR20120079281A - A novel flavimycin compound having peptide deformylayse inhibition and antibacterial activity - Google Patents

Abstract

PURPOSE: A novel flavimycin compound and an antibacterial composition containing the same are provided to treat infectious diseases by superbacteria. CONSTITUTION: An antibacterial composition contains a compound of chemical formula 1 or 2, or isomer, derivative, or pharmaceutically acceptable salt thereof. The compound is prepared from Aspergillus flavipes F020543 strain(KCTC 10880BP). The composition has an antibacterial activity against Staphylococus aureus, Bacillus subtilis, Staphylococcus epidermis, methicillin-resistant Staphylococcus aureus(MRSA), or quinolone-resistant Staphylococcus aureus(QRSA). A composition for suppressing peptide diformylase activity contains the compound of chemical formula 1 or 2. A method for preparing the compound of chemical formula 1 or 2 comprises: a step of culturing Aspergillus flavipes F020543 strain(KCTC 10880BP) or mutant strain thereof; a step of extracting the strain culture liquid and mycelium with an organic solvent; and a step of performing chromatography of the ethyl acetate extract.

Description

A novel flavimycin compound having peptide deformylayse inhibition and antibacterial activity

The present invention uses the novel pravimycin compound represented by the formula (1) or (2), an antimicrobial composition comprising the same as an active ingredient, a composition for inhibiting peptide deformillase activity, and an Aspergillus prabibs F020543 strain. It relates to a manufacturing method.

Hospital microbial genome research, which began in the mid-1990s, has uncovered new antibiotic targets, opening up the possibility of developing new concepts. One of the new antibiotic targets identified and validated using microbial genome information is the protein biosynthetic peptide Peformide deformylase (PDF). Bacteria are bound to tRNA for protein synthesis, and then formylated by transformylase. After protein synthesis is completed, formyl groups drop by PDF to become active proteins. As such, PDF is an enzyme that is essential for bacterial growth and is present in most pathogens, and the antimicrobial spectrum is a good antibiotic target with a broad spectrum. In addition, in humans, similar genes are present in mitochondria but are found to have no function and are known to be low in human toxicity (Drug Discovery Today 6 (18) 954-961, 2001).

PDFs are also known to exist in Apicomplexa, such as the Plasmodium falciparum, which causes malaria. In fact, the existing PDF inhibitor actinonin (actinonin) has been reported to inhibit the growth of tropical heat worms, PDF inhibitor is also promising as a treatment for malaria.

The known PDF inhibitors include actinone, a peptide compound with hydroxamate functional groups, and actinone, a reverse hydroxamate functional group, developed by the multinational pharmaceutical company Novartis, actinone) derivative compounds LBM-415 and BB-83698 are known (Curr. Med. Chem. 12: 1607-1621, 2005).

However, the compounds have good in vitro antimicrobial activity, but because they are peptide compounds, they have problems with human absorption and stability in the human body.

Accordingly, the present inventors have made diligent efforts to develop a substance which inhibits the activity of PDF from the metabolite of a microorganism. As a result, the present inventors have found a fungus producing a substance that strongly inhibits the PDF, and at the same time, characterized the microbiological characteristics of the producing strain. The present invention was completed by purely separating and purifying new PDF activity inhibitory substance from the culture medium of the strain, and then determining the chemical structure and examining and confirming the activity.

It is an object of the present invention to provide an antimicrobial composition comprising a compound represented by Formula 1 or Formula 2, an isomer thereof, a derivative thereof or a pharmaceutically acceptable salt thereof.

Another object of the present invention is to provide a composition for inhibiting peptide deformylase activity, which comprises a compound represented by Formula 1 or Formula 2.

Another object of the present invention to provide an antimicrobial composition for antimicrobial comprising a compound represented by the formula (1) or (2) as an active ingredient.

Another object of the present invention is to provide a compound represented by the formula (1) or (2).

Another object of the present invention is to provide a method for producing the compound.

In order to achieve the above object, the present invention as one embodiment provides an antimicrobial composition comprising a compound represented by the following formula (1) or (2), isomers, derivatives or pharmaceutically acceptable salts thereof.

[Formula 1: Pravimycin A]

[Formula 2: Prabimycin B]

Compounds of the present invention include prabimycin A and B, as well as isomers, derivatives or pharmaceutically acceptable salts thereof. The prabimycin compound is a newly discovered and identified compound by the present inventors, and exhibits excellent antimicrobial activity.

In the present invention, the 'isomer' refers to a relationship between compounds having the same chemical formula but not identical, and the kind of such isomers includes structural isomers, geometric isomers, optical isomers, and geometric isomers. A stereoisomer means a compound having the same chemical composition but different in terms of the arrangement of atoms or groups in space, and an optical isomer (enantiomer) means two stereoisomers of a compound having mirror images that do not overlap each other, and diastereomers Isomers refer to stereoisomers that have two or more asymmetric centers and whose molecules are not mirror images of each other.

In the present invention, "derivative" means a compound obtained by substituting a part of the structure of a prabimycin A or B compound with another atom or group of atoms, and a "pharmaceutically acceptable salt" means a relatively non-toxic inorganic and organic acid of the compound. It means addition salt.

The compounds of the present invention have excellent peptide deformillase inhibitory activity. In one embodiment of the present invention, the enzyme inhibitory ability of prabimycin A and B against peptide deformillase (PDF) of Staphylococcus aureus, an exemplary major pathogen, was measured. As a result, prabimycin A was measured. IC ₅₀ of B and 35.8μM and 32.1μM, respectively, it was confirmed that strongly inhibit the PDF activity (Example 3 and Table 3). These results support that the compound of the present invention can be used as an antimicrobial composition.

In addition, since the compound of the present invention strongly inhibits the activity of PDF, it can be usefully used for the prevention or treatment of malaria caused by Plasmodium falciparum.

The compounds of the present invention can be synthesized according to methods commonly used in the art, and can also be obtained as natural compounds produced from strains. The compound of the present invention is preferably Aspergillus flavipes ) , and more preferably from the Aspergillus prabib F020543 strain (Accession Number: KCTC 10880BP).

As another aspect, the present invention provides a method for treating an infectious disease caused by a pathogenic microorganism or resistant bacteria, comprising administering the antimicrobial composition of the present invention to a subject having an infectious disease caused by the pathogenic microorganism or resistant bacteria.

As used herein, the term "treatment" means any action that improves or advantageously changes the symptoms caused by an infectious disease caused by a pathogenic microorganism or a resistant bacterium by administration of a pharmaceutical composition. In the present invention, the term "individual" refers to a pathogenic microorganism or Means all animals, including humans that have developed or can infect infectious diseases caused by resistant bacteria, and by administering the pharmaceutical composition of the present invention to an individual, the disease can be effectively treated.

In the present invention, the pathogenic microorganisms are all microorganisms that cause disease or harm while invading the living organisms of animals and plants, and include bacteria, yeasts and fungi of Gram-positive bacteria and Gram-negative bacteria, preferably Staphylococcus aureus. Reus, Staphylococcus epidermis, Bacillus subtilis or Candida albicans.

In the present invention, the resistant bacteria means that the bacterium exhibits resistance to antibiotics as a result of continuous use of the drug to treat or prevent any disease and its complications or any bacterial disorders and complications thereof. Examples of such antibiotics include cephalosporins, quinolones and fluoroquinolones, penicillins, beta lactamase inhibitors, carbepenems, monobactams, macrolides and lincosamines, glycopeptides, rifampins, oxazolidinones, tetracyclines, aminoglycoses Seeds, streptogramamine and sulfonamides, and antibiotic-resistant bacteria are resistant even when the antibiotics listed above are treated, so that the disease is maintained continuously in the subject, preferably MRSA (methicillin-resistant Staphylococcus aureus) or QRSA ( Quinolone-resistant Staphylococcus aureus).

In one embodiment of the present invention, the antimicrobial activity of prabimycin A and B against Staphylococcus aureus, Staphylococcus epidermis, Bacillus subtilis, MRSA and QRSA was measured. , Prabimycin A and B showed potent antimicrobial activity against each bacterium (32 μg / ml MIC, Example 4 and Table 4). Therefore, the compounds of the present invention can be usefully used for the prevention or treatment of infectious diseases caused by pathogenic microorganisms or resistant bacteria.

The antimicrobial composition of the present invention may contain not only the compound of the present invention but also one or more known active ingredients having antimicrobial activity against pathogenic bacteria.

In addition, the antimicrobial composition of the present invention may further include a pharmaceutically acceptable carrier.

The term "pharmaceutically acceptable carrier" in the present invention refers to liquid or solid fillers involved in the transport or transport of any subject composition or component from one organ or part of the body to another organ or part of the body. Refers to a pharmaceutically acceptable material, composition or vehicle, such as a diluent, excipient, solvent or encapsulating material, wherein the composition of the present invention further comprises a pharmaceutically acceptable carrier, excipient or diluent in addition to the active ingredients described above for administration. It may include. The carrier, excipient and diluent may include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, Polyvinyl pyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil.

In addition, the antimicrobial compositions of the present invention may be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols, oral formulations, external preparations, suppositories, or sterile injectable solutions according to conventional methods. Can be used. Specifically, when formulated, it may be prepared using conventional diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents, and surfactants. Solid preparations for oral administration include, but are not limited to, tablets, pills, powders, granules, capsules, and the like. Such solid preparations may be prepared by mixing at least one excipient such as starch, calcium carbonate, sucrose, lactose, gelatin and the like with the compound of Formula 1 or 2. In addition to simple excipients, lubricants such as magnesium stearate and talc may also be used. Liquid preparations for oral use include, but are not limited to, suspending agents, solvents, emulsions, syrups, and the like, and various excipients, such as wetting agents, sweeteners, fragrances, It can be prepared by adding a preservative or the like. Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations and suppositories. As the non-aqueous solvent and suspending agent, propylene glycol, polyethylene glycol, vegetable oils such as olive oil, injectable esters such as ethyl oleate and the like can be used. As the base of the suppository, utopsol, macrogol, tween 61, cacao butter, laurin butter, glycerogelatin and the like can be used.

In addition, the compositions of the present invention can be administered orally or parenterally (eg, intravenously, subcutaneously, intraperitoneally or topically) according to the desired method, and the dosage is determined by the condition and weight of the patient, disease Depending on the degree, drug form, route of administration, and duration, it may be appropriately selected by those skilled in the art. It may be administered once or several times daily as needed, and used alone or in combination with methods using surgery, hormone therapy, drug treatment and biological response modifiers for the prevention or treatment of pathogenic bacteria and resistant bacteria. Can be.

As another aspect, the present invention provides a composition for inhibiting peptide deformylase activity comprising the compound represented by the formula (1) or (2).

Bacteria are bound to tRNA for protein synthesis by methionine, and then formylated by transformylase. After protein synthesis is completed, formyl groups drop to become active proteins. At this time, the formyl group is dropped by the peptide deformillase to become an active protein.

The peptide deformylase is known to be present in most pathogens while being an enzyme necessary for the growth of bacteria. Peptide deformylase is also known to be present in Apicomplexa, such as the Plasmodium falciparum, which causes malaria.

In one embodiment of the present invention it was confirmed that the compound represented by the formula (1) or (2) has inhibitory activity against peptide deformillase (Example 3 and Table 3).

As another aspect, the present invention provides an antimicrobial composition for antimicrobial comprising the compound represented by the formula (1) or formula (2) as an active ingredient. That is, the present invention provides a quasi-drug composition for the purpose of preventing or improving infectious diseases caused by pathogenic microorganisms or resistant bacteria.

The quasi-drug composition of the present invention can be used together with other quasi-drugs or quasi-drug components, and can be suitably used according to a conventional method. The mixed amount of the active ingredient may be appropriately determined depending on the purpose of use (prevention, health or therapeutic treatment).

The quasi-drug composition may be a disinfectant cleaner, a shower foam, a gagreen, a wet tissue, a detergent soap, a hand wash, a humidifier filler, a mask, an ointment, or a filter filler.

As another aspect, the present invention provides a prabimycin A represented by the formula (1) or a prabimycin B compound represented by the formula (2).

The prabimycin is a novel compound obtained by culturing Aspergillus prabibs F020543 strain, obtained as a white powder, prabimycin A is a novel compound having a molecular formula of C ₁₈ H ₁₈ O ₉ , a molecular weight of 378, Prabimycin B is a novel compound with a molecular formula of C ₁₉ H ₂₀ O ₁₀ , having a molecular weight of 408.

In another embodiment, the method comprises the steps of: culturing Aspergillus prabibs F020543 strain (KCTC 10880BP) or a mutant thereof; 2) extracting the culture medium and mycelium of the strain obtained in step 1) with an organic solvent and then extracting with ethyl acetate; And performing chromatography on the ethyl acetate extract obtained in step 2) to obtain a compound of the present invention.

When the step 1) is described in detail, the general properties of the mold are not constant, but are easily changed naturally or artificially, and the Aspergillus prapips F020543 strain of the present invention is also easy to change its properties. Thus, the strain may include the Aspergillus prabbius F020543 strain, as well as strains newly produced by mutant strains (natural or mutagenic strains), conjugates or genetic engineering methods derived from the strains.

The culture of Aspergillus prabibs F020543 strain or mutant strain thereof is cultured in a medium containing nutrients that can be used by conventional microorganisms. As a nutrient source, the well-known nutrient source currently used for the cultivation of a mold is used. For example, as a carbon source, glucose, starch syrup, dextrin, starch, molasses, animal oil, vegetable oil, etc. may be used, and as nitrogen sources, bran, soybean meal, wheat, malt, cottonseed gourd, fishmeal, corn steep liquor, gravy, yeast Extracts, ammonium sulfate, sodium nitrate, urea and the like can be used. If necessary, it is very effective to add salts, potassium, magnesium, cobalt, chlorine, phosphoric acid, sulfuric acid and other inorganic salts that promote ion generation. As a culture method, shaking culture or political culture is possible under aerobic conditions.

The culture temperature is slightly different depending on the conditions when the culture in each of the above conditions, it is usually suitable to incubate at 20 ~ 37 ℃, in most cases it is incubated at 26 ~ 30 ℃. In addition, in the culture period of shaking and stationary culture, the production of the prabimycin compound of the present invention reached the highest when usually cultured for 4 days to 7 days.

Step 2) is a step of extracting the culture medium and mycelia of the Aspergillus prabibs F020543 strain or a mutant strain thereof, the prabimycin compound is present in the mycelia portion as well as the culture solution of the strain. Therefore, by adding an organic solvent such as acetone to the culture medium and mycelium of the strain, extracting the active ingredient from the culture medium and the mycelium, acetone is evaporated under reduced pressure, solvent extraction with ethyl acetate, and the ethyl acetate solvent layer is concentrated under reduced pressure to remove ethyl acetate. do.

Step 3) is a step of separating the compound of the present invention, the purification and separation of the compound can be used without limitation the methods commonly used in the art, if necessary, the type of medium, culture conditions, extraction purification method, etc. It is obvious that the yield and yield can be controlled by changing the. In one embodiment of the present invention, the compound of the present invention was prepared by performing chromatography on ethyl acetate extract by the following method.

The ethyl acetate concentrate obtained in step 2) was subjected to silica gel column chromatography using chloroform: methanol at 20: 1 to 1: 1 to concentrate the active fraction under reduced pressure to obtain an oily crude active ingredient, and then methanol as a solvent. Purification on Sephadex LH-20 column chromatography. Finally, the active fractions were subjected to HPLC under a solvent condition of methanol: water = 30: 70 to obtain two pure compounds, prabimycin A and B (Example 2).

The compound of the present invention strongly inhibits the activity of PDF, has a strong antimicrobial activity against pathogenic microorganisms and antibiotic resistant bacteria, and particularly shows a strong antimicrobial activity against the antibiotic resistant bacteria MRSA and QRSA, so as to treat infectious diseases caused by superbacteria This can be useful for.

1 is a view showing the chemical structural formula of prabimycin A according to the present invention.
Figure 2 is a view showing the chemical structural formula of pravimycin B according to the present invention.
3 is a graph showing the PDF inhibitory activity of prabimycin A.

Hereinafter, the present invention will be described in more detail with reference to Examples and Experimental Examples. However, the following examples are merely to illustrate the present invention is not limited to the contents of the present invention.

Example  One : Aspergillus flavipes F020543  Isolation of strain

The present inventors isolated the fungus F543 having a peptide deformillase inhibitory activity from the fungal strains after screening the fungus to isolate the strain producing a substance having a peptide deformillase inhibitory activity. The F543 strain is conidia small and smooth-walled, conidia pale grayish orange when viewed on a plate, and conidia on biseriate aspergilli (which forms conidia on metulae and phialide). Aspergillus flavipes (Bain. & Sart.) Thom & Church 1926 was identified as the point of formation, which was named Aspergillus flavipes F543. The present inventors deposited the strain at the Genetic Resource Center, Korea Research Institute of Bioscience and Biotechnology, December 9, 2005 (Accession Number: KCTC 10880BP).

Example  2 : Aspergillus flavipes F020543  From strain Fravimycin  Separation and Purification

2-1. Aspergillus flavipes F020543  Culture of strain

To cultivate the Aspergillus flavipesF020543 strain, species medium containing 0.3% yeast extract, 0.3% malt extract, 0.5% tryptone, 1% glucose before pH sterilization It was used after adjusting to 5.5.

A 100 ml Erlenmeyer flask containing 20 ml of the seed medium was sterilized at 121 ° C. for 20 minutes, inoculated with 1 platinum from a slope culture tube of Aspergillus flavipesF020543 strain, and incubated at 28 ° C. for 3 days. Used as a culture. Then, the seed culture solution was inoculated into a 500 ml Erlenmeyer flask containing 48 sterile media and incubated at 28 ° C. for 7 days.

2-2. Aspergillus flavipes F020543  From strain Fravimycin  Separation and Purification

The acetone extract of the culture medium and mycelium cultured in Example 2-1 was solvent extracted three times with ethyl acetate. The ethyl acetate solvent layer containing the active ingredient thus obtained was concentrated under reduced pressure to remove ethyl acetate, and then silica gel column chromatography was performed using chloroform: methanol as a solvent having 20: 1-1: 1. The active fraction thus obtained was concentrated under reduced pressure to obtain an oily crude active ingredient, which was then purified by Sephadex LH-20 column chromatography using methanol as a solvent. Finally, the active fractions were subjected to HPLC in a solvent condition of methanol: water = 30: 70 to separate prabimycin A and B.

The physicochemical characteristics of pravimycin A and B isolated from the Aspergillus flavipesF020543 strain were as follows.

Compound 1: Pravimycin  A

1) Physical property: white powder;

2) molecular weight: 378;

3) High Resolution ESI-MS:

Found m / z 377.0874 (MH) ⁻ (C ₁₈ H ₁₇ O ₉ ), calcd 377.0878;

4) Molecular Formula: C ₁₈ H ₁₈ O ₉ ;

5) UV absorption spectrum [UV (MeOH) λ max (logε)]: 211 (4.38), 271 (3.14) nm;

6) IR spectrum: 3397, 1631, 1317, 1021 cm ⁻¹ ;

7) Nuclear Magnetic Resonance (NMR) Data: ¹ H and ¹³ C NMR data using dimethyl sulfoxide (DMSO-d ₆ ) as a solvent are shown in Table 1 below.

8) Chemical Structural Formula

Compound 2: Pravimycin  B

1) the appearance of the substance: white powder;

2) molecular weight: 408;

3) High Resolution ESI-MS:

Found m / z 377.0874 (MH) ⁻ (C ₁₉ H ₂₀ O ₁₀ ), calcd. 377.0878;

4) Molecular Formula: C ₁₉ H ₂₀ O ₁₀ ;

5) UV absorption spectrum [UV (MeOH) λ max (logε)]: 211 (4.38), 271 (3.14) nm;

6) IR spectrum: 3397, 1631, 1317, 1021 cm ⁻¹ ;

7) Nuclear Magnetic Resonance (NMR) Data: ¹ H and ¹³ C NMR data using dimethyl sulfoxide (DMSO-d ₆ ) as a solvent are shown in Table 2 below.

8) Chemical Structural Formula

Example  3: Pravimycin  Peptide deformillase of compounds ( Peptide deformylase , PDF) Inhibition activity measurement

In order to confirm the PDF inhibitory activity of prabimycin according to the present invention, the following enzyme titer assay was performed.

A PDF-FDH (formate dehydrogenase) coupled assay was constructed to measure enzyme titers. Staphylococcus aureus PDF prepared by genetic recombination technology was used. Titer measurements were performed in 50 mM HEPES buffer (pH 7.5), and as a substrate, N-fromylmethionine-alanine-serine (f-MAS) 4 mM, NAD 2 mM, BSA 1 mg / ml, PDF was 30 -50 nM was used and FDH was 0.05 Unit. After the enzyme was added and reacted at room temperature for 60 minutes, the absorbance of NADH (nicotinamide adenine dinucleotide) was measured at 340 nm using a UV-spectrophotometer. Compounds evaluated for inhibition were dissolved in dimethyl sulfoxide (DMSO) solvent and added within 5% of the total reaction solution to evaluate enzyme inhibition. Enzyme inhibition capacity was expressed as a percentage of the NADH increase of the test compound to the increase in NADH increase in the absence of the test compound, and the concentration of each test compound that inhibited 50% of enzyme activity was determined as IC ₅₀ . The results are shown in Table 3, and the graph of PDF inhibition activity of prabimycin A is shown in FIG.

compound IC ₅₀ ([mu] M) Phramycin A 35.8 Pravimycin B 32.1

As shown in Table 3, the IC ₅₀ for peptide deformillase of prabimycin A and B is Excellent peptide deformylase inhibitory activity was shown as 35.8 μM and 32.1 μM, respectively (Table 3). In addition, as shown in Figure 3, pramycin A shows peptide deformylase inhibitory activity of 26% at 10μM, 46% at 30μM, 50% at 35.8μM, 69% at 100μM, and activity of peptide deformillase in a concentration-dependent manner. Strongly inhibited (FIG. 3).

Example  4 : Pravimycin  Determination of Antimicrobial Activity of Compounds

In order to confirm the antimicrobial activity of the prabimycin compound according to the present invention, the following experiment was performed.

The test strain was cultured in Mueller Hinton broth (MHB), and the antimicrobial activity was measured by broth micro dilution. After diluting the test bacteria incubated overnight to 2 x 100,000 / ㎖, dispense 100 μl per well in 96 well plate, and actinin (frainomycin A, B and positive control) Treatment was carried out with 2-fold dilution gradually from concentrations up to 128 μg / ml. Each compound was diluted in DMSO, and the experiment was performed to adjust the concentration of DMSO to approximately 1/100. After incubation for 20 hours, the growth of bacteria was examined by measuring the OD value at 650 nm. The minimum concentration of the compound which completely inhibited the growth of bacteria was determined by MIC, and the results are shown in Table 4 below.

MIC (μg / ml) S. aureus MRSA3167 QRSA3505 B. subtilis S. epidermis Phramycin A 32 32 64 32 32 Pravimycin B 32 32 32 32 32 Actinine 32 32 32 32 32

As shown in Table 4, the prabimycin A and B compounds of the present invention showed excellent antibacterial activity against S. aureus, a major pathogen (32 μg / ml MIC), in particular antibiotics. It also showed excellent antimicrobial activity against the resistant bacteria MRSA (methicillin-resistant Staphylococcus aureus) and QRSA (Quinolone-resistant Staphylococcus aureus). Similar antimicrobial activity was also observed for B. subtilis and S. epidermis (32 μg / ml MIC, Table 4).

Korea Biotechnology Research Institute KCTC10880BP 20051209

Claims (10)

An antimicrobial composition comprising a compound represented by Formula 1 or Formula 2, an isomer thereof, a derivative thereof, or a pharmaceutically acceptable salt thereof.
[Formula 1]

(2)

The composition of claim 1, wherein the compound is produced from Aspergillus flavipes F020543 strain (KCTC 10880BP).
The method of claim 1, wherein the composition is Staphylococus aureus, Bacillus subtilis, Staphylococcus epidermis, Methicillin-resistant staphylococci (methicillin-resistant) Staphylococcus aureus (MRSA) and Quinolone-resistant Staphylococcus aureus (QSA) composition that exhibits antimicrobial activity against any one or more bacteria selected from the group consisting of. The composition of claim 1, wherein the compound has a peptide deformylase inhibitory activity.
The composition of claim 1, wherein the composition further comprises a pharmaceutically acceptable carrier.
A composition for inhibiting peptide deformylase activity comprising a compound represented by Formula 1 or Formula 2.
[Formula 1]

(2)

The method of claim 6, wherein the composition is Staphylococus aureus, Bacillus subtilis, Staphylococcus epidermis, Methicillin-resistant staphylococci (methicillin-resistant) Staphylococcus aureus (MRSA) and Quinolone-resistant Staphylococcus aureus (QSA) A composition that exhibits antimicrobial activity against any one or more bacteria selected from the group consisting of.
Antimicrobial quasi-drug composition comprising the compound represented by the following formula (1) or (2) as an active ingredient.
[Formula 1]

(2)

A compound represented by the following formula (1) or (2).
[Formula 1]

(2)

1) culturing the Aspergillus prabiles F020543 strain (KCTC 10880BP) or a mutant thereof;
2) extracting the culture medium and mycelium of the strain obtained in step 1) with an organic solvent and then with ethyl acetate; And
3) A method for preparing a compound according to claim 9, comprising the step of obtaining the compound of claim 9 by chromatography on the ethyl acetate extract obtained in step 2).

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