Tetrahydro carboline derivative modified with two amino acids and preparation method and application thereof

Abstract

The invention discloses a tetrahydro carboline derivative modified with two amino acids and a preparation method and an application thereof. According to the invention, L-tryptophan methyl ester is allowed to react with 1,1,3,3-tetramethoxy propane by a microwave reaction; the obtained product is modified by amino acids to obtain a series of (1R, 3S)-1-[1-(1R, 3S)-tetrahydro beta-carboline-3-formyl amino acid-1-yl-methyl]-tetrahydro beta-carboline-3-formyl amino acid derivatives and intermediates thereof; and the derivatives are evaluated for in vitro antiplatelet aggregation activity and in vitro antithrombotic activity. The method of the invention is simple; the used raw materials are easily available, safe and cheap; the obtained product has antiplatelet aggregation activity and antithrombotic activity, which indicates the clinical application prospects of (1R, 3S)-1-[1-(1R, 3S)-tetrahydro beta-carboline-3-formyl amino acid-1-yl-methyl]-tetrahydro beta-carboline-3-formyl amino acidas an antithrombotic agent.

Description

technical field The present invention relates to an antithrombotic drug, in particular to (1R, 3S)-1-[1-(1R, 3S)-tetrahydroβ-carboline-3-formyl amino acid-1-yl-methyl]-tetrahydro The hydrogen β-carboline-3-formyl amino acid derivative and its preparation method and application belong to the field of biomedicine. Background technique Thrombotic disease is a common cardiovascular and cerebrovascular disease, often manifested as myocardial infarction, ischemic cerebral infarction, and venous thromboembolism. Every year, 1 to 3 people per 1,000 people suffer from different forms of thrombotic disease, seriously affecting human health. At present, antithrombotic and thrombolytic drugs commonly used in clinical practice have various shortcomings, such as bleeding, gastric mucosal injury, liver injury and other side effects. It is the goal of drug researchers to find antithrombotic drugs that are safer, more effective, and less toxic. one. It is generally believed that the form...

AI Technical Summary

Problems solved by technology

(3S)-1,2,3,4-tetrahydrocarboline-3-carboxylic acid has been known to have antiplatelet activity, but poor water solubility and fat solubility make the bioavailability very low, so it must carry out structural transformation