Preparation of substituted indole lactam derivative and application of substituted indole lactam derivative as antimalarial agent

Abstract

The invention designs an efficient synthesis method for preparing a compound shown as a general formula (I) and an application of a derivative of the compound to the research and development of an antimalarial active medicament. The method comprises the following steps of: dissolving a reactant into an appropriate solvent; and reacting under the irradiation condition of a high-voltage mercury lamp (ultraviolet lamp). In the method disclosed by the invention, a series of poly-substituted indole lactam compounds taking 3,4,5-trisubstituted indole as a basic framework are efficiently synthesized with a one-pot method under an illumination condition, so that the defects of complex steps, difficulty in operating and low total yield existing in synthesis of the type of compounds under the condition of the prior art are overcome. Derivatives containing different substituted functional groups are obtained only through a four-step reaction, and the type of compounds has potential antimalarial activity, so that necessary material bases are provided for the researches of active screening, acting mechanisms and structure-activity relationships of a large quantity of analogues, and the type of compound can possibly become a new type of antimalarial candidate medicament. The general formula (I) is shown in the specifications.

Description

Technical field

[0001] The invention relates to a preparation method of a multi-substituted indololactam derivative characterized by 3,4,5-tri-substituted indole and its use as an antimalarial agent in the research and development. The invention belongs to the field of biomedicine. Background technique

[0002] Malaria is a global acute parasitic disease that is caused by Plasmodium and is transmitted by Anopheles mosquitoes. There are 4 species of Plasmodium that infect humans, namely Plasmodium falciparum, Plasmodium vivax, Plasmodium vivax and Plasmodium ovale. Among them, Plasmodium falciparum is the main pathogen of malaria in sub-Saharan Africa, and it is also the Plasmodium causing the highest mortality in patients. The life history of Plasmodium is very complicated. The spore stage of Plasmodium enters the human body through mosquito bites, first invades the liver, and matures into schizonts in the liver cells. As the liver cells burst, the released merozoites enter the...

Images