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Preparation method for terpyridine pyridinium complex and application thereof in reverse transcriptase inhibition

A technology of ruthenium terpyridine and terpyridine, which is applied in the field of HIV reverse transcriptase inhibitor research and development, can solve the problems of lack of light absorption, fluorescence and other spectral properties, low water solubility, etc., and achieve good spectral properties, stable structure, and good water solubility. Effects of Sex and Stability

Inactive Publication Date: 2018-12-28
YUNNAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as an organic small molecule compound, its water solubility is low, and it lacks applicable spectral properties such as light absorption and fluorescence.

Method used

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  • Preparation method for terpyridine pyridinium complex and application thereof in reverse transcriptase inhibition
  • Preparation method for terpyridine pyridinium complex and application thereof in reverse transcriptase inhibition
  • Preparation method for terpyridine pyridinium complex and application thereof in reverse transcriptase inhibition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 3

[0046] Example 1 Preparation of terpyridine ruthenium (II) complexes

[0047] The molecular structure of the synthesized terpyridine ruthenium (II) complex is as follows: figure 1 shown.

[0048] 1. Precursor complex [Ru(tpy)Cl 3 ] Preparation:

[0049] Precursor complex [Ru(tpy)Cl 3 ]according to figure 2 The indicated pathways were synthesized. Weigh 2-acetylpyridine (12.1 g, 0.1 mol) into a round bottom flask, add N,N-dimethylformamide dimethyl acetal (24.0 g, 0.2 mol) and 500 mL xylene, reflux for 4 hours . Xylene was distilled off under reduced pressure, and yellow crystals were obtained by recrystallization from n-pentane. The crystals were added to a solution of potassium tert-butoxide (23.0 g, 0.2 mol) and 2-acetylpyridine (12.1 g, 0.1 mol) in 500 mL of anhydrous tetrahydrofuran, and the reaction solution changed from bright yellow to pinkish yellow. Stir for 4 hours, add ammonium acetate (77.0 g, 1 mol) and acetic acid (250 mL), and stir for 5 minutes. All ...

Embodiment 2

[0058] Example 2 UV-visible detection of ruthenium(II) complexes interacting with RNA

[0059]The configuration of the solution adopts the weighing method. The solvent is twice distilled water, and the buffer system is Tris-NaCl, pH 7.0. The concentration of the terpyridine ruthenium(II) complex is 2×10 -5 mol / L, poly(A) RNA and DNA concentration range is about 5×10 -6 ~5×10 -5 mol / L, the concentration of DNA or poly(A) RNA was gradually increased in the solution of fixed concentration of terpyridine ruthenium(II) complex, and the UV-vis spectra of the complex itself and different RNA concentrations were recorded respectively. Such as Figure 7 As shown, with the increase of DNA or poly(A) RNA concentration, the UV-visible spectrum of the terpyridine ruthenium(II) complex RuTz1 basically did not change, while the UV-visible spectra of RuTz2 and RuTz3 increased with the addition of poly(A) RNA The change is obvious, but basically unchanged with the addition of DNA. This...

Embodiment 3

[0060] Example 3 Recognition effect of terpyridine ruthenium (II) complex on HIV RNA

[0061] Gel electrophoresis was used to test the recognition effect of terpyridine ruthenium (II) complexes on the TAR region of HIV RNA. In a 0.2 mL PCR tube, prepare a series of 10 μL solutions containing 2×10 -6 mol / L TAR RNA, 2×10 -6 mol / L tat polypeptide, and 0~5×10 -5 mol / L terpyridine ruthenium (II) complex. The solution was incubated at 37°C for 30 minutes, 2 μL of RNA electrophoresis loading buffer was added, and electrophoresis was performed on a 10% polyacrylamide gel (denatured with urea) at 110 V for 1 hour. After staining with Gelred 4S nucleic acid dye for 15 minutes, take pictures with a gel imager and analyze the electrophoretic bands. Such as Figure 8 As shown, HIV TAR RNA itself shows a band. In the presence of tat polypeptide, part of the TAR RNA and the tat polypeptide are hydrogen bonded, so that electrophoresis shows two bands, that is, TAR RNA that is not boun...

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Abstract

The invention belongs to the field of research and development of HIV inhibitors, and discloses a preparation method for a terpyridine pyridinium (II) complex and application thereof in HIV reverse transcriptase inhibition. The structure of a cationic moiety of the terpyridine pyridinium (II) complex is as shown in a formula I. A preparation process for the terpyridine pyridinium (II) complex is optimized, the raw material cost is low, and the reaction time is short. The obtained complex is high in purity and yield and has good water solubility and excellent spectral properties. The terpyridine pyridinium (II) complex has the capability of selective binding to a TAR region on HIV RNA, and can block the reverse transcription process of viral RNA by reverse transcriptase and inhibit the replication of viral RNA. The terpyridine pyridinium (II) complex is a highly affinitive HIV RNA selective binding reagent and a highly active HIV reverse transcriptase inhibitor, and is an HIV drug having a great application potential.

Description

technical field [0001] The invention belongs to the field of research and development of HIV reverse transcriptase inhibitors, in particular to a preparation method of ruthenium terpyridine complex and its application in HIV reverse transcriptase inhibition. Background technique [0002] AIDS is the most devastating epidemic in human history. Since 2015, AIDS has become the number one infectious disease death in my country. There is currently no drug or therapy in the world that can cure AIDS. In December 2015, the latest report of the World Health Organization (WHO) pointed out that reverse transcriptase inhibitors are currently the most promising drugs to cure AIDS. A large number of experiments have proved that inhibiting the reverse transcription of viral RNA by reverse transcriptase can control the production and spread of the virus, and play a role in the treatment and early prevention of AIDS ( science , 1992, 256 , 1783-1790; Biochemistry , 2011, 50 , 5042-505...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P31/18G01N21/31G01N27/447
CPCA61P31/18C07F15/0046G01N21/31G01N27/447
Inventor 高峰马国兰毕徐丹
Owner YUNNAN UNIV
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