Bithiophene compound and pharmaceutical composite and application thereof

A bithiophene compound technology, applied in organic chemistry, antibacterial drugs, pharmaceutical formulations, etc., can solve the problems of complex components, difficult separation, and no bithiophene compounds with antibacterial activity, and achieve good antibacterial activity Effect

Inactive Publication Date: 2010-06-09
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such thiophenes contained in Compositae plants are relatively complex, and their content is low, and there is great difficulty in separation, and there are certain restrictions on development and utilization. Therefore, the research on Compositae plants should focus...

Method used

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  • Bithiophene compound and pharmaceutical composite and application thereof
  • Bithiophene compound and pharmaceutical composite and application thereof
  • Bithiophene compound and pharmaceutical composite and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of Compound 1-10:

[0045] 1. Extraction and separation:

[0046] 20kg of the whole herb of Xinjiang blue thorn head, dried and crushed, refluxed with 95% industrial ethanol for 3 times, 4 hours each time, the extract was concentrated under reduced pressure to obtain an extract, which was dissolved in water and then extracted 3 times with petroleum ether. Extracted three times with ethyl acetate, concentrated under reduced pressure to obtain the extract, and finally extracted three times with n-butanol saturated with water; the ethyl acetate part was eluted with a gradient of chloroform-methanol solvent system to obtain six fractions of Fr1-Fr6, Fr2 The four fractions of -Fr5 were separated by repeated silica gel column chromatography, the eluent was petroleum ether: acetone (100:0-50:50) gradient elution, and the gel LH-20 was chromatographically separated, and the eluent was chloroform: Methanol (50:50) and repeated RP-18 reverse-phase silica gel column c...

Embodiment 2

[0059] Tablet: Compound 1 obtained in Example 1 10mg, lactose 180mm, starch 55mg, magnesium stearate 5mg;

[0060] Preparation method: mix compound 1, lactose and starch, wet evenly with water, sieve the wet mixture and dry it, then sieve it, add magnesium stearate, and then press the mixture into tablets, each tablet weighs 250 mg, and the compound content is 10 mg.

Embodiment 3

[0062] Ampoule: 22 mg of the compound obtained in Example 1, 10 mg of sodium chloride;

[0063] Preparation method: Dissolve compound 2 and sodium chloride in an appropriate amount of water for injection, filter the resulting solution, and fill it into an ampoule bottle under sterile conditions.

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PUM

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Abstract

The invention relates to bithiophene compounds shown in a general formula (I) and a preparation method and applications thereof, wherein the R1 is -H, -CHO, -COOH, -CHOHCH2OH, -CH2OH or -CH3 and R2 is -H, -1-propyne, -4-hydroxy-1-butyne, -3,4-dihydroxy-1-butyne or -COCH2CH2CH2OH.

Description

Technical field: [0001] The invention belongs to the field of compounds with antibacterial activity, and in particular relates to a class of bithiophene compounds with antibacterial activity, its pharmaceutical composition, its preparation method and its application in antibacterial agents. Background technique: [0002] Natural thiophene compounds mainly exist in Compositae. A series of monothiophenes, dithiophenes, triple thiophenes and their derivatives have been isolated from Compositae plants. These metabolites have a wide range of biological activities. Such as: cytotoxicity, anti-HIV, insecticide, antibacterial. Such thiophenes contained in Compositae plants are relatively complex, and their content is low, and there is great difficulty in separation, and there are certain restrictions on development and utilization. Therefore, the research on Compositae plants should focus on the selection of active, And those with high active ingredient content are the research obj...

Claims

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Application Information

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IPC IPC(8): C07D407/14C07D333/38C07D333/16C07D333/22A61K31/381A61P31/04A61P31/10
Inventor 朱华结李良波任洁
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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