A kind of antifungal compound containing thiazole and its preparation method and application
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The technology of a compound, azole, is applied in the field of medicine to achieve the effect of high yield, good effect and strong antifungal activity
Inactive Publication Date: 2016-05-11
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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But so far no azole compound N-alkyl-N-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-trifluorophenyl) with antifungal activity Reports on oxazol-1-yl))-propyl-aminodithiocarbamic acid benzyl ester or its salts
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Embodiment 1
[0033] The preparation of embodiment 1 compound of the present invention
[0035] 1-[2-(2,4-difluorophenyl)-2,3-epoxypropyl]-1H-1,2,4-triazole mesylate 21g, with methylamine 10mL, triethylamine 20mL, heat and reflux in 300mL ethanol for 6-8 hours, distill off the solvent after the reaction is complete, extract with 200mL ethyl acetate, wash with 100mL×2 water, dry over anhydrous sodium sulfate, filter, distill off ethyl acetate to obtain oily 1- (1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-methylamino)-2-ol 11.96g, yield 68.0% .
[0036] Preparation of N-methyl-N-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl))-propyl-amino Benzyl dithioformate (compound 6a in Table 1):
[0037] In a 50mL single-neck bottle, put a magnet, add 10mL absolute ethanol, 0.536g 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)- 3-(N-Methylamino)-2-ol (2 mmol). After 10 min of ice-water bath, ...
Embodiment 2
[0124] The pharmacological experiment of embodiment 2 compounds of the present invention
[0125] (1) Experimental method
[0126] Conventional in vitro antibacterial test methods are used, see: AntimicrobAgentsChemother1995,39(5):1169 for details.
[0127] (1) Experimental strains
[0128] In this experiment, the following 8 common human pathogenic standard fungal strains were selected as screening objects:
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Abstract
The invention is a sulfur / nitrogen-containing azole antifungal compound as well as a preparation method and an application of the sulfur / nitrogen-containing azole antifungal compound, relates to the technical field of medicine. The sulfur / nitrogen-containing azole antifungal compound is a novel azole antifungal compound and has a chemical structural formula which is shown in the specification, wherein, R1 is hydrogen or a straight-chain or branched-chain saturated or unsaturated lower alkyl having 1-6 carbon atoms; R2 is selected from hydrogen, alkyl, halogen, cyano group, a nitro group, an amino and an alkoxy, can be located at the ortho, meta or para position of the benzene ring and can be monosubstituted or polysubstituted. The invention also provides a preparation method and an application of the compound. The compound disclosed by the invention has strong antifungal activity on the deep fungal, has the advantages of high efficiency, low toxicity, broad anti-fungal spectrum and the like compared with the current clinically applied antifungal drugs, and therefore, the compound can be used for the preparation of efficient antifungal agents.
Description
technical field [0001] The invention relates to the field of medical technology, and is a novel nitrogen azole antifungal compound—N-alkyl-N-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2, 4-triazol-1-yl))-propyl-aminodithiocarbamic acid benzyl ester compounds and salts thereof, as well as their preparation methods and uses. Background technique [0002] In recent years, with the widespread application of broad-spectrum antibiotics, antineoplastic drugs, and immunosuppressants, the widespread development of peritoneal dialysis, organ transplantation, and radiotherapy, and the rapid spread of immunodeficiency diseases, especially AIDS, Candida albicans, Cryptography neoformans The incidence of opportunistic deep fungal infections such as coccus and Aspergillus fumigatus has increased dramatically. Deep fungal infection has risen to the third largest infectious disease clinically, seriously threatening human life and health. Most of the antifungal drugs currently in clinical us...
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Patent Type & Authority Patents(China)
IPC IPC(8): C07D249/08A61K31/4196A61P31/10
CPCC07D249/08
Inventor 邹燕潘炜华廖万清赵庆杰胡宏岗吴秋业吴茂诚李翔潘博宋阳俞世冲柴晓云
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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