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Application of dodecyl diamine derivatives in preparation of medicines for treating AIDS

A technology of lauryl diamine and derivatives, which can be used in antiviral agents, pharmaceutical formulas, medical preparations containing active ingredients, etc., and can solve problems such as drug resistance and non-responsiveness

Inactive Publication Date: 2019-02-26
柴梦莹
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the development of drugs and the continuous growth of virus resistance, problems such as great drug resistance and non-response have emerged in its application.

Method used

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  • Application of dodecyl diamine derivatives in preparation of medicines for treating AIDS
  • Application of dodecyl diamine derivatives in preparation of medicines for treating AIDS
  • Application of dodecyl diamine derivatives in preparation of medicines for treating AIDS

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0065] Experimental example 1 Inhibition of the binding of the test compound to the 12G5 antibody CXCR4 receptor

[0066] CXCR4 is a receptor heavily expressed by lymphocytes and leukocytes in a steady state, and the physiological function of this receptor will determine the activity, differentiation, migration and immune regulation of cells. SDF-1 is a natural chemokine and agonist of CXCR4. Therefore, by effectively inhibiting the binding of CXCR4 to SDF-1, the signaling of CXCR4 can be regulated to maintain normal cell physiological functions and avoid hematopoietic differentiated cells (immune cells and leukocytes). AMD3100 is a class of adjuvant anticancer drugs that can effectively activate lymphocyte activation. It also has a strong ability to inhibit CXCR4 signaling and inhibit CXCR4-tropic HIV invasion. However, its main defect for AIDS indications is that it inhibits CXCR4 The signal is too strong, completely blocking the physiological function of the host lymphocyt...

experiment example 2

[0077] Experimental example 2 Specific recognition experiment of test compound to CXCR4

[0078] CCR5 receptor is a special chemokine receptor expressed by T lymphocytes in the activated state. For T lymphocytes, both CXCR4 and CCR5 are induced to express when they are activated or activated by various signals. CXCR4 and CCR5 sometimes aggregate into heterodimers, and irregular binding can lead to changes in membrane receptor signaling and complete changes in cell physiological functions. Therefore, in order to confirm the CXCR4-specific recognition ability of the three cinnamic diamine derivatives in the present application and its specific inhibition of CXCR4 subtype virus, but not CCR5 subtype virus specific inhibition, this experiment was carried out.

[0079] In order to confirm the binding specificity of the test compound to CXCR4 but not to CCR5, the inventors chose to use A3.01-R5T lymphocytes, which express both CXCR4 and CCR5 receptors. Membrane protein labeling wi...

experiment example 3

[0087] Experimental example 3 Specific recognition experiment of test compound on SDF-1 binding to CXCR4

[0088] The expression of CXCR4 and CXCR7 receptors is a molecular basis for the migration, activation, bundling and effector of lymphocytes. Does the test compound use the CXCR4 or CXCR7 receptor expressed on the cell membrane as a target? Specifically inhibit the binding of SDF-1 to CXCR4 or CXCR7? This is an important indicator to prove that the test compound targets the CXCR4 antagonist.

[0089] SDF-1 can specifically recognize CXCR4 and CXCR7. In order to confirm that the lauryl diamine derivatives in this application can specifically block the binding of SDF-1 to CXCR4, but not to CXCR7, the inventors demonstrated through the following experiments.

[0090] 1. Experimental principle

[0091] SDF-1 will be coupled to Tebium reagent (signal ligand), and Tebium reagent will be used in HTRF homologous Ford energy transfer experiments; while CXCR4 and CXCR7 will be co...

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Abstract

Application of dodecyl diamine derivatives in preparation of medicines for treating AIDS is provided, belonging to the field of antivirus medicines. The inventor found that the dodecyl diamine derivatives shown as a formula I, a formula II and a formula III can powerfully inhibit the invasion of lymphocytes by the AIDS type I CXCR4 tropic virus strain, and prevent the strain from attacking and destroying the immune system, with the acquired immune deficiency syndrome being caused by the virus strain, thus indicating that the three compounds can specifically target CXCR4 and efficiently suppress infection of the AIDS type I CXCR4 tropic virus, can be used as an anti-AIDS therapeutic drugs for first-line invasion inhibitors and have a wide application prospect.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the application of a lauryl diamine derivative in the preparation of medicines for treating AIDS. Background technique [0002] Since AIDS (AIDS) was first discovered in 1981, the medical community has not yet successfully developed a method that can completely treat AIDS, nor has it successfully produced a vaccine to prevent human immunodeficiency virus (also known as HIV AIDS virus) infection, but developed Many drugs and methods inhibit the reverse transcriptase (RT), block the replication of HIV, and slow down the growth rate of the virus. [0003] There are two types of AIDS, HIV-I and HIV-II. Among them, type II HIV mainly reproduces in several African countries such as West Africa, and its sensitivity and pathogenicity are relatively low. Type I HIV is the main strain prevalent in the world and is divided into 3 subtype groups. General clinical anti-HIV drugs mainly act against...

Claims

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Application Information

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IPC IPC(8): A61K31/4178A61P31/18
CPCA61K31/4178A61P31/18
Inventor 周志诚柴梦莹
Owner 柴梦莹