CN108864043A - A kind of preparation method and purposes of novel quinolone compounds - Google Patents
A kind of preparation method and purposes of novel quinolone compounds Download PDFInfo
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Abstract
The invention discloses a kind of novel quinolone compounds, preparation method and purposes.The novel quinolone compounds have following structures：
Description
Technical field
The invention belongs to organic syntheses and drug field, and in particular to a kind of for treating the novel quinolone of bacterium infection
Compound, preparation method and purposes, more particularly to by the way that balofloxacin and acyl chlorides or anhydride reaction are prepared 11- acyl groups
Application of the novel quinolone compounds and this novel quinolone compounds replaced in preparation antibacterials.
Background technique
Balofloxacin (structural formula sees below formula) is a kind of forth generation carbostyril family antibacterial drugs, clinically for treating bladder
Inflammation, urethritis etc.[1]。
Antibacterial activity in vitro experiments have shown that, Balofloxacin has gram-positive bacteria, Gram-negative bacteria and anaerobic bacteria
The bacteriostatic activity of wide spectrum.It is slightly weaker than tosufloxacin for the antimicrobial effect of gram positive bacteria, than Norfloxacin, Ofloxacin, ring
Third husky star and Lomefloxacin are all strong；Balofloxacin is more husky than Norfloxacin, Ofloxacin, cyclopropyl to the antimicrobial effect of gram-negative bacteria
Star and tosufloxacin are weak, suitable with Lomefloxacin.Wherein, to the Methicillin Sensitive Staphylococcus aureus being clinically separated
(MSSA), methicillin-resistant staphylococcus aureus (MRSA), staphylococcus epidermis, streptococcus pneumonia and streptococcus pyogenes
MIC90Respectively 0.2,6.25,0.2,0.39 and 0.39 (μ g/ml)[2].Therefore, clinically it is mainly used for as caused by pathogenic bacteria
Pneumonia, pulmonary suppuration disease etc. especially have very strong bacteriostasis to pneumonia caused by mycoplasma, Chlamydia etc.[3-5]。
Although Balofloxacin is the fluoroquinolone antibiotics of a new generation, there is also some shortcomingss, such as：To leather
Blue positive cocci effect is weaker, and additionally there are some gastrointestinal tracts, central nervous system symptom and allergic reaction, clinical blood is raw
Change and checks visible slight serum transaminase and aspartate transaminase rising and Eosinophilia etc.[2,6].Therefore,
Structural modification can be carried out to Balofloxacin and obtain the novel quinolone compounds of high-efficiency low-toxicity, expand its application.
Currently, the report of balofloxacin structural modification transformation is relatively fewer, the acylation that we mainly pass through 11 is introduced
The side-chain radical of different length, improves the dissolubility of Balofloxacin, while the bioavilability of compound being made to get a promotion, antibacterial
Activity is also improved to some extent.
Bibliography
[1]Alksne L.Balofloxacin Choongwae[J].Curr Opin Investig Drugs,2003,4
(2): 224-229.
[2] in vitro activity [J] medicine Leader of Chen Jing, Wu Yong Balofloxacin, 2006,25 (11)：
1126-1128.
[3] more than seedling, the external medical antibiotic fascicle of Guo Hui member broad spectrum quinolone class antimicrobial balofloxacin [J], 2004,
25(2)：79-82.
[4]Nakashima M,Uematsu T,Fukuchi M,et al.Clinical phase Ⅰ study of
balofloxacin Ⅰ.Single oral administration[J].Japanese journal of
chemotherapy,1995,43(S5): S115-S140.
[5]Nakashima M,Uematsu T,Fukuchi M,et al.Clinical phase Ⅰ study of
balofloxacin Ⅱ.Repeated oral adminstration[J].Japanese journal of
chemotherapy,1995,43(S5): S141-S159.
[6] Mi Zhiyuan, Liu Wanzhong new fluoroquinolones Balofloxacin progress [J] Chinese Journal of New Drugs,
2005,14 (9)：1205-1210.
Summary of the invention
The purpose of the present invention is to provide a kind of for treating the novel quinolone compounds of bacterium infection.
A second object of the present invention is to provide a kind of preparation methods of novel quinolone compounds.
A kind of purposes third object of the present invention is to provide novel quinolone compounds as antibacterials.
The purpose of the present invention is what is be achieved through the following technical solutions：
A kind of novel quinolone compounds have following structures：
Wherein, R=CH3Or N=0-10.
A kind of preparation method of novel quinolone compounds, it is characterized in that according to 1：2-1：4 by Balofloxacin and acyl chlorides or
Anhydride reaction, obtains novel quinolone compounds, and the novel quinolone compounds have following structures：
Wherein, R=CH3Or N=0-10.
A kind of application of novel quinolone compounds in preparation antibacterials.
Novel quinolone compounds of the invention have good antibacterial activity, and has a broad antifungal spectrum, targeting is strong, biofacies
Capacitive is good, and bioavilability is high, and toxicity is low；And preparation method is simple, quick, high income, is suitable for large-scale industrialization
Production.
Detailed description of the invention
Fig. 1 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 1.
Fig. 2 is the high resolution mass spectrum figure of the novel quinolone compounds of the embodiment of the present invention 1.
Fig. 3 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 2.
Fig. 4 is the high resolution mass spectrum figure of the novel quinolone compounds of the embodiment of the present invention 2.
Fig. 5 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 3.
Fig. 6 is the high resolution mass spectrum figure of the novel quinolone compounds of the embodiment of the present invention 3.
Fig. 7 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 4.
Fig. 8 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 5.
Fig. 9 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 6.
Figure 10 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 7.
Figure 11 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 8.
Figure 12 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 9.
Figure 13 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 10.
Figure 14 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 11.
Figure 15 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 12.
Figure 16 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 13.
Figure 17 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 14.
Figure 18 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 15.
Figure 19 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 16.
Figure 20 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 17.
Figure 21 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 18.
Figure 22 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 19.
Figure 23 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 20.
Figure 24 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 21.
Figure 25 is the synthetic route of the novel quinolone compounds of the embodiment of the present invention 22.
Specific embodiment
Below by embodiment, the invention will be further described, and purpose, which is only that, better understands the contents of the present invention
The protection scope being not intended to limit the present invention：
The synthesis of 1 methyl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 10mL formic acid is added in room temperature, is at the uniform velocity stirred to react 10min, slowly
200 μ L of formaldehyde is added dropwise, 100 DEG C are heated to reflux, and stirring for 24 hours, the water of 2 times of volumes, methylene chloride extraction, water is added into reaction solution
It washes three times, organic phase is concentrated, cold ether is precipitated precipitating, obtains novel 0.17 g of quinolone compounds, yield after concentration
82.13% (synthetic route is shown in that Fig. 1, characterization map are shown in Fig. 2).
The synthesis of 2 acetyl group Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
141 μ L of 208 μ L of triethylamine and chloroacetic chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 3 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, after concentration be precipitated precipitating, obtain novel quinoline promise
Ketone compound 0.15g, yield 67.57% (synthetic route is shown in that Fig. 3, characterization map are shown in Fig. 4).
The synthesis of 3 propiono Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
90 μ L of 190 μ L of triethylamine and propionyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 4 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, concentration, obtain novel quinolone compounds
0.14g, yield 61.14% (synthetic route is shown in that Fig. 5, characterization map are shown in Fig. 6).
The synthesis of 4 formoxyl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 10mL formic acid is added in room temperature, at the uniform velocity it is stirred to react 10min, 110
It DEG C is heated to reflux, stirring for 24 hours, the water of 2 times of volumes, methylene chloride extraction is added into reaction solution, and washing three times, is concentrated organic
Phase, cold ether, concentration obtain novel quinolone compounds 0.07g, yield 33% (synthetic route is shown in Fig. 7).
The synthesis of 5 bytyry Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
104 μ L of 100 μ L of triethylamine and butyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 3 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, concentration, obtain novel quinolone compounds
0.16g, yield 67.80% (synthetic route is shown in Fig. 8).
The synthesis of 6 valeryl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
122 μ L of 100 μ L of triethylamine and valeric chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 4 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, concentration, obtain novel quinolone compounds
0.10g, yield 41.18% (synthetic route is shown in Fig. 9).
The synthesis of 7 caproyl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
132 μ L of 100 μ L of triethylamine and caproyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 2 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, after concentration be precipitated precipitating, obtain novel quinoline promise
Ketone compound 0.12g, yield 47.92% (synthetic route is shown in Figure 10).
The synthesis of 8 heptanoyl group Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
142 μ L of 100 μ L of triethylamine and oenanthyl chloro, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 3 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, after concentration be precipitated precipitating, obtain novel quinoline promise
Ketone compound 0.09g, yield 34.94% (synthetic route is shown in Figure 11).
The synthesis of 9 caprylyl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
159 μ L of 100 μ L of triethylamine and caprylyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 4 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, concentration, obtain novel quinolone compounds
0.13g, yield 49.09% (synthetic route is shown in Figure 12).
The synthesis of 10 pelargonyl group Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
190 μ L of 100 μ L of triethylamine and pelargonyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 2 times of volumes of addition into reaction solution
Water, methylene chloride extraction, washing three times, be concentrated organic phase, cold ether, concentration, obtain novel quinolone compounds
0.15g, yield 55.15% (synthetic route is shown in Figure 13).
The synthesis of 11 certain herbaceous plants with big flowers acyl group Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
205 μ L of 100 μ L of triethylamine and certain herbaceous plants with big flowers acyl chlorides is added dropwise, 0 DEG C of stirring 30min is stirred at room temperature for 24 hours, 3 times of volumes of addition into reaction solution
Three times, organic phase, cold ether is concentrated in water, methylene chloride extraction, washing, and concentration obtains novel quinolone compounds
0.12g, yield 42.98% (synthetic route is shown in Figure 14).
The synthesis of 12 cyano Balofloxacin derivative of embodiment
1.1g cyanoacetic acid is taken to be dissolved in anhydrous methylene chloride, -10 DEG C of stirring 10min are slowly added to 1.04 mL of oxalyl chloride
With the DMF of catalytic amount, end of reaction, Rotary Evaporators remove oxalyl chloride and solvent, and product, which is added, contains 0.389g Balofloxacin
DMF solution in, add 200 μ L triethylamines, react at room temperature 12h, the water of 4 times of volumes, methylene chloride are added into reaction solution
Three times, organic phase is concentrated in extraction, washing, and cold ether is precipitated precipitating, obtains novel quinolone compounds 0.1g after concentration,
Yield 22.10% (synthetic route is shown in Figure 15).
The synthesis of 13 alanine Balofloxacin of embodiment
It takes 0.15mg boc- alanine to be dissolved in 5mLDMF, stirs 5min, 232 μ L of triethylamine and ethyl chloroformate 151 is added
μ L, is stirred to react 30min, adds the DMF solution 25mL of the balofloxacin containing 0.2g, is stirred to react for 24 hours, is added into reaction solution
The water of 2 times of volumes, methylene chloride extraction, washing three times, are concentrated organic phase, 10mL trifluoroacetic acid are added, is stirred to react 12h, subtracts
Pressure removes trifluoroacetic acid, and ether washing obtains novel quinolone compounds 0.2g, (synthetic route is shown in figure to yield 69.47%
16)。
The synthesis of 14 triazole Balofloxacin of embodiment
0.389g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, delays
Slow to be added dropwise 153 μ L of chloracetyl chloride, 0 DEG C of stirring 30min, room temperature is stirred for for 24 hours, and the water of 3 times of volumes, generation are added into reaction solution
A large amount of insoluble matters are stirred for 1h, and filtering, filter cake dries to obtain intermediate 0.34g, yield 73.12%.0.1g intermediate is weighed,
It is dissolved in 10mL acetonitrile, adds 22mg triazole sodium, 50 DEG C of reaction 48h, concentration of reaction solution, silica gel column chromatography obtains novel quinoline promise
Ketone compound 0.07g, yield 58.33% (synthetic route is shown in Figure 17).
The synthesis of 15 cyclopropyl acyl group Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
120 μ L of 108 μ L of triethylamine and cyclopropyl acyl chlorides, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 4 times of bodies of addition into reaction solution
Three times, organic phase is concentrated in long-pending water, methylene chloride extraction, washing, and cold ether is precipitated precipitating, obtains novel quinoline after concentration
Promise ketone compound 0.15g, yield 67.57% (synthetic route is shown in Figure 18).
The synthesis of 16 ring valeryl Balofloxacin of embodiment
It takes 0.1g cyclopentanecarboxylic acid to be dissolved in 5mL DMF, stirs 5min, 134 μ L of triethylamine and 100 μ L of ethyl chloroformate is added,
It is stirred to react 30min, the DMF solution 20mL of the balofloxacin containing 0.24g is added, is stirred to react for 24 hours, 3 are added into reaction solution
Three times, organic phase is concentrated in the water of times volume, methylene chloride extraction, washing, and precipitating is precipitated in cold ether after concentration, obtain new
Type quinolone compounds 0.2g, yield 66.82% (synthetic route is shown in Figure 19).
The synthesis of 17 cyclohexanoyl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, 0 DEG C of addition 10mL DMF is at the uniform velocity stirred to react 10min, slowly
150 μ L of 107 μ L of triethylamine and Cyclohexanoyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 4 times of bodies of addition into reaction solution
Three times, organic phase, cold ether is concentrated in long-pending water, methylene chloride extraction, washing, and concentration obtains novel quinolone compounds
0.22g, yield 85.94% (synthetic route is shown in Figure 20).
The synthesis of 18 benzoyl Balofloxacin of embodiment
0.2g Balofloxacin is taken, is set in a round bottom flask, the DMF of 0 DEG C of addition 10mL is at the uniform velocity stirred to react 10min, slowly
150 μ L of 107 μ L of triethylamine and chlorobenzoyl chloride, 0 DEG C of stirring 30min is added dropwise, room temperature is stirred for for 24 hours, 2 times of bodies of addition into reaction solution
Three times, organic phase, cold ether is concentrated in long-pending water, methylene chloride extraction, washing, and concentration obtains novel quinolone compounds
0.22g, yield 70.87% (synthetic route is shown in Figure 21).
The synthesis of 19 pyridine -3- formoxyl Balofloxacin of embodiment
It takes 0.1g Nicotinicum Acidum to be dissolved in 5mLDMF, stirs 5min, triethylamine 261 μ L and 170 μ of ethyl chloroformate is added
L is stirred to react 30min, adds the DMF solution 20mL of the balofloxacin containing 0.2g, is stirred to react for 24 hours, 3 are added into reaction solution
Three times, organic phase, cold ether is concentrated in the water of times volume, methylene chloride extraction, washing, and concentration obtains novel quinolone
Close object 0.18g, yield 58.06% (synthetic route is shown in Figure 22).
The synthesis of 20 2- furanylcarbonyl Balofloxacin of embodiment
It takes 0.1g niacin to be dissolved in 5mLDMF, stirs 5min, 147 μ L of triethylamine and 75 μ L of ethyl chloroformate is added, stirring is anti-
30min is answered, the DMF solution 20mL of the balofloxacin containing 0.2g is added, is stirred to react for 24 hours, 4 times of volumes are added into reaction solution
Three times, organic phase is concentrated in water, methylene chloride extraction, washing, and cold ether is precipitated precipitating, obtains novel quinolone after concentration
Compound 0.2g, yield 78.74% (synthetic route is shown in Figure 23).
The synthesis of 21 2- tetrahydrofuran formoxyl Balofloxacin of embodiment
It takes 0.1g 2- tetrahydrofuran formic acid to be dissolved in 5mLDMF, stirs 5min, 252 μ L of triethylamine and ethyl chloroformate is added
164 μ L, are stirred to react 30min, add the DMF solution 20mL of the balofloxacin containing 0.24g, are stirred to react for 24 hours, into reaction solution
The water of 2 times of volumes, methylene chloride extraction is added, three times, organic phase is concentrated in washing, and cold ether is precipitated precipitating, obtains after concentration
To novel quinolone compounds 0.21g, yield 70.02% (synthetic route is shown in Figure 24).
The synthesis of 22 pyrroles's -2- formoxyl Balofloxacin of embodiment
0.1g 2- pyrrole carboxylic acid 5mL DMF is taken, 5min is stirred, 125 μ L of triethylamine and 94 μ L of ethyl chloroformate is added, stirs
Reaction 30min is mixed, the DMF solution 20mL of the balofloxacin containing 0.25g is added, is stirred to react for 24 hours, 4 times are added into reaction solution
Three times, organic phase is concentrated, cold ether, concentration, silica gel column chromatography obtains novel in the water of volume, methylene chloride extraction, washing
Quinolone compounds 0.21g, yield are 67.74% (synthetic route is shown in Figure 25).
The research of the novel quinolone compounds antibacterial activity of embodiment 23
According to 1-22 of the embodiment of the present invention method prepare novel quinolone compounds in-vitro antibacterial pharmacodynamic evaluation,
Include the following steps：
(1) experimental strain
Methicillin-resistant staphylococcus aureus (MRSA), pseudomonas aeruginosa (P.aeru) are selected in this experiment
ATCC27853 and escherichia coli (E.coli) ATCC25922 is provided as screening object by 304 hospital of Beijing.
(2) experimental method
Bacteria suspension is prepared：With aseptic manipulation, after taking 3 kinds of freeze-drying standard strains to restore room temperature, with plate streak, difference
Straight line is drawn in 3 LB solid medium tablets, 37 DEG C of culture 18h are distinguished according still further to fluid nutrient medium inocalation method with oese
Dip bacterium, culture transferring shakes in tube in 3 LB liquid mediums containing 5mL, and 37 DEG C of culture 16h of 180rpm shaking table pass through enzyme mark
Instrument detection, is diluted to 1 × 10 for bacterium solution6CFU/mL is spare.
Drug solution preparing：The novel quinolone compounds for taking 1-22 of the embodiment of the present invention to prepare are dissolved in dimethyl sulfoxide, are made into 10
The medicine storage liquid of mg/mL, -20 DEG C of preservations, is configured to 40 for drug by doubling dilution with LB liquid medium before experiment,
20,10,5,2.5,1.25,0.63,0.31,0.16,0.08,0.04,0.02,0.01,0.005μg/mL。
Inoculation：According to the standard of the American National Clinical Laboratory Standard committee, using doubling dilution in 96 orifice plates
Novel quinolone compounds are evaluated to the in vitro anti-microbial activity of three kinds of bacteriums (MRSA, P.aeru and E.coli).Take 180 μ
L medical fluid and 20 μ L bacterium solutions are separately added into 96 orifice plates, are mixed.Blank group is 200 μ L fluid nutrient mediums, and growth control group is 180 μ
L fluid nutrient medium and 20 μ L bacterium solutions.Sample is protected from light incubation for 24 hours at 37 DEG C, observes the muddy degree of bacterium solution, first appearance is muddy
It is turbid reduce, the drug concentration of solution clear is minimal inhibitory concentration (MIC).Then, the bacterium solution of 100 μ L is drawn respectively,
Even to be coated on LB solid medium, 37 DEG C are protected from light incubation for 24 hours, observe bacterium colony growing state, clump count≤5 in each culture dish
Drug concentration be minimum bactericidal concentration (MBC).
(3) experimental result
Antibacterial experiment in vitro the results are shown in Table 1.
The experimental results showed that novel quinolone compounds of the invention have preferable antibacterial activity, to methicillin-resistant
Staphylococcus aureus and Pseudomonas aeruginosa show the novel quinoline of good fungistatic effect, especially embodiment 2 and embodiment 3
Promise ketone compound antibacterial effect is better than balofloxacin, the especially antibacterial activity of acetyl group Balofloxacin, to the MIC of three bacterial strains
Respectively 0.02,0.04,2.50 μ g/mL, MBC are respectively 0.04,0.08,5.00 μ g/mL, have good antibacterials exploitation
Prospect.
The antibacterial activity (μ g/mL) of the novel quinolone compounds of table 1
Claims (3)
1. a kind of novel quinolone compounds, it is characterized in that having following structures：
Wherein, R=CH3Or
2. a kind of preparation method of novel quinolone compounds, it is characterized in that according to 1：2-1：4 by Balofloxacin and acyl chlorides or acid
Anhydride reactant, obtains novel quinolone compounds, and the novel quinolone compounds have following structures：
Wherein, R=CH3Or
3. a kind of application of the novel quinolone compounds described in claim 1 in preparation antibacterials.
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