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Candida albicans-resistant medicines with unsaturated fatty acid structure and preparation method of candida albicans-resistant medicines

A technology of unsaturated fatty acids and Candida albicans, which is applied in the direction of antifungal agents, can solve the problems of high toxicity of bromination reagent liquid bromine, expensive methyl lithium, cumbersome operation, etc., and achieve short synthesis routes, precise routes, Simple operation effect

Inactive Publication Date: 2015-04-29
NANJING UNIV OF POSTS & TELECOMM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the synthesis of DSF drugs requires at least three steps (such as III), the selected raw material fatty acid needs to be obtained by industrial production, methyllithium is expensive, and the bromination reagent liquid bromine is more toxic and seriously pollutes the environment. Not only the cost is high, but also cumbersome operation

Method used

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  • Candida albicans-resistant medicines with unsaturated fatty acid structure and preparation method of candida albicans-resistant medicines
  • Candida albicans-resistant medicines with unsaturated fatty acid structure and preparation method of candida albicans-resistant medicines
  • Candida albicans-resistant medicines with unsaturated fatty acid structure and preparation method of candida albicans-resistant medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Step 1. In a two-necked round bottom flask (100mL), add sodium azide (0.975g, 15mmol), potassium iodide (0.083g, 0.5mmol), nitrogen protection, add dimethyl sulfoxide 15mL, nitrogen protection, at 50°C Stir. Then, bromooctane (1.92 g, 10 mmol) was added to the reaction system. After the dropwise addition, continue to stir at 50°C for 10h. The reaction was quenched with ice water, extracted with petroleum ether, the organic phase was washed with water and saturated sodium chloride solution, dried over anhydrous sodium sulfate, and concentrated to obtain 1.3 g of octane azide with a yield of 87%.

[0029] Step 2. Add sodium ascorbate (0.17g, 0.85mmol) into a two-neck round bottom flask (100mL) under nitrogen protection. Then 3 mL of ethanol was added. Nitrogen was blown, and 3 mL of an aqueous solution of copper sulfate (0.1 g, 4 mmol) was added, and then propiolic acid (0.73 g, 10 mmol) and octane azide (1.35 g, 8.7 mmol) were added dropwise to react for 5 h. The rea...

example 2- example 6

[0031] Example 2-Example 6, method is the same as Example 1, and the specific experimental consumption is as follows:

[0032] Step 1

[0033] R 1 R 1 Br (g, mmol) NaN 3 (g, mmol) KI (g, mmol) DMSO (mL) R 1 N 3 (g) Yield(%) 2 C 6 h 13 1.64,10 0.975,15 0.083,0.5 15 0.9 70 3 C 6 h 12 Oh 1.80,10 0.975,15 0.083,0.5 15 0.9 63 4 C 12 h 25 2.50,10 0.975,15 0.083,0.5 15 1.4 70 5 C 8 h 17 1.92,10 0.975,15 0.083,0.5 15 1.4 90 6 C 8 h 17 1.92,10 0.975,15 0.083,0.5 15 1.3 84

[0034] Step 2

[0035]

[0036] characterizing data

[0037] Product 2:

[0038]

[0039] 1 H NMR (400MHz, DMSO) δ (ppm): 11.0 (s, 1H), 8.68 (s, 1H), 4.45–4.31 (m, 2H), 1.87–1.73 (m, 2H), 1.22 (pd, J= 8.0,5.0Hz,6H),0.82(t,J=7.0Hz,3H).

[0040] Product 3:

[0041]

[0042] 1 H NMR (400MHz, DMSO) δ (ppm): 11.2 (s, 1H), 8.27 (s, 1H), 4.34 (t, J = 14.1, 7.2Hz, 2H), 1.80 (m, J = 31.2, 23.7Hz ,2H),1.4...

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Abstract

The invention discloses a method for rapidly preparing and screening candida albicans-resistant medicines with an unsaturated fatty acid structure. A structure of an analogue or a derivative of a class of the candida albicans-resistant medicines is represented by a formula (II), wherein R1 represents one of linear alkyl, terminal hydroxyl or sulfydryl-substituted alkyl, oligomeric polyethylene glycol or 1,4-alkyl piperazine; R2 represents one of hydroxyl, amino and methoxyl; and the characters of the medicines are screened by virtue of a bactericidal experiment. The invention discloses a preparation method and a screening method of synthesized medicines. According to the preparation method and the screening method, the development cost of a new medicine can be lowered, and the detection efficiency of the new medicine can be effectively improved.

Description

technical field [0001] The invention belongs to the field of drug design and drug screening, and specifically relates to the field of preparation of a class of anti-candida albicans drugs. Background technique [0002] Candida albicans (Candida albicans) is a common opportunistic fungus in humans and one of the main pathogens of clinically acquired infections. Under normal circumstances, it exists in the form of symbiotic bacteria on the skin, oral cavity, gastrointestinal tract and mucosal surface of the human body. When the human immune system is normal, Candida albicans, as a symbiotic bacterium, maintains a balance with other microbial flora in the body and will not cause disease infection. However, when immunity is weakened or antibacterial drugs are overused, it may rapidly expand on the mucosal surface and cause Candidiasis. The most common clinically are oral candidiasis and candidal vaginitis. In addition, Candida can enter endothelial cells through tissue damage...

Claims

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Application Information

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IPC IPC(8): C07D249/04A61P31/10
CPCC07D249/04
Inventor 汪联辉何聪傅妮娜翁丽星伍开翔
Owner NANJING UNIV OF POSTS & TELECOMM
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