1-(3-aminopropyl) piperazine-4-aminoamide compound as well as preparation method and application thereof

Abstract

The invention discloses a 1-(3-aminopropyl) piperazine-4-aminoamide compound as well as a preparation method and application thereof. The structural general formula of the compound is shown as a formula I, wherein R1 is the following groups unsubstituted or substituted by 1-3 substituents: phenyl groups, benzyl groups, naphthyl groups, C5-C10 aromatic heterocyclic groups or C4-C7 saturated heterocyclic groups; the heterocyclic groups comprises 1-3 (at least 1) heteroatoms selected from N, O and S; the substituents are selected from the following atoms or groups: halogen, sulfydryl groups, hydroxyl groups, CF3, CN, NO2 and SO2CH3; and X is methylene, carbonyl or does exist. Through cell activity screening of an HIV-1 infected Bal(R5) lymphoid tissue sample, the series of compound is found to have very strong anti-HIV (Human Immunodeficiency Virus) activity, wherein the compound with strongest activity has the IC50 value reaching 10nM and the selection index more than 14.545 and can be developed into anti-AIDs medicaments. The formula I is shown in the specification.

Description

technical field The invention relates to 1-(3-aminopropyl)piperazine-4-aminoamide compounds, their preparation method and application. Background technique AIDS (AIDS) is a disease caused by human immunodeficiency virus (HIV) infection, mainly manifested by immune deficiency. Since the first case of AIDS was reported in the United States in 1981, AIDS has become the infectious disease that has caused the most deaths in the world. The advent of cocktail therapy has greatly reduced the mortality rate of HIV-1 infected persons. However, HIV-1 has developed drug resistance to almost all current antiviral drugs, and antiviral drugs generally have disadvantages such as high toxicity. Therefore, it is still an important task to discover and develop anti-HIV drugs with definite mechanism of action and novel structure types. The CCR5 receptor, a member of the chemokine receptor family, is an important co-receptor for HIV-1 to enter cells. In some people who are resistant to R5 HI...

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Problems solved by technology

However, HIV-1 has developed resistance to almost all current antiviral drugs, and antiviral drugs generally have disadvantages such as high toxicity

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