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Synthetic method and application of a class of novel mycobacterial inhibitors

A technology for mycobacteria and uses, applied in the field of medicine, can solve problems such as no compounds that inhibit ester acyl-CoA synthase, and achieve the effect of good clinical application prospects

Inactive Publication Date: 2020-06-30
SICHUAN NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, there are no reports of compounds that inhibit this type of acyl-CoA synthetase

Method used

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  • Synthetic method and application of a class of novel mycobacterial inhibitors
  • Synthetic method and application of a class of novel mycobacterial inhibitors
  • Synthetic method and application of a class of novel mycobacterial inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation method of embodiment 1 inhibitor P1 (formula II)

[0035] synthetic route:

[0036]

[0037] The preparation method of compound 5, it comprises the following steps:

[0038] Step 1: Under the protection of argon, add adenosine (10.0g), DMF (40mL), imidazole (22.0g) and tert-butyldimethylsilyl chloride (50g) into a round bottom bottle in turn, at 40 degrees Celsius The reaction was stopped after stirring for 13 h. Dichloromethane was added for extraction, and the organic layer was sequentially washed with saturated NaHCO 3 、H 2 O was washed several times, dried and filtered, concentrated under reduced pressure, and column chromatography gave light yellow oily liquid compound 1.

[0039] Step 2: Weigh compound 1 (10g), 80% CH 3 COOH (100mL) was placed in a round-bottomed flask, refluxed at 100°C for 5h, then stopped the reaction, adjusted the pH to 8 with saturated NaOH, extracted with ethyl acetate, washed the organic layer several times with wate...

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PUM

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Abstract

The invention discloses a compound of formula I as shown in the specification, or an optical isomer, a pharmaceutically acceptable salt, hydrate or a solvate of the compound. R1 and R2 are respectively independently selected from hydrogen and hydroxyl. The compound and the salt, the hydrate or the solvate of the compound, which are disclosed by the invention, are special inhibitors of mycobacteria, the inhibitors are capable of specially inhibiting enzymatic activity of acyl coenzyme A synthetase which joins in side chain degradation of a steroid compound, have efficient inhibition activity upon growth of mycobacterium smegmatis, mycobacterium neoaurum, mycobacterium murinum, mycobacterium fortuitum, mycobacterium tuberculosis and the like, and have no inhibition function on escherichia coli and brewer's yeast.

Description

technical field [0001] The invention relates to the field of medicine, in particular, the invention relates to the design and synthesis of a class of mycobacterial selective novel inhibitors. Background technique [0002] Pathogenic bacteria in the Mycobacterium genus cause a variety of infectious diseases in hosts ranging from fish to humans. The World Health Organization estimates that approximately three million people die from tuberculosis each year worldwide, and more than eight million people are infected with Mycobacterium tuberculosis (WHO, 2009). In addition, studies in recent years have shown that non-tuberculous mycobacteria in the genus Mycobacterium also seriously threaten and endanger the life and health of humans and animals. There are more than 150 non-tuberculous mycobacteria found so far, and the pathogenic bacteria or conditions Pathogenic bacteria account for about 1 / 3, and the more common types include Mycobacterium avium intracellulare complex, Mycobac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J43/00A61K31/58A61P31/06
CPCA61P31/06C07J43/003Y02A50/30
Inventor 李维葛方兰牛杨任尧陈贵英
Owner SICHUAN NORMAL UNIV
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