Binary Conjugate for Thrombolysis and Radical Scavenging
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Solution Overview
Problem
Current thrombotic drugs have limitations, including high effective dosages, lack of verification for anti-thrombotic and free radical scavenging activities, and limited efficacy in treating stroke beyond 30 minutes from onset, necessitating a compound with thrombolytic, anti-thrombotic, and free radical scavenging functions that can cross the blood-brain barrier effectively at a low dose.
Innovation Solution
A novel binary conjugate formed by coupling a thrombolytic oligopeptide and a tetrahydroisoquinoline compound with C1-4 alkyl groups via a linking arm, creating a nanostructure that enhances stability, crossing efficiency, and free radical scavenging capabilities, allowing for effective thrombolysis and antithrombotic activity at low doses.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional thrombotic drugs are used, then thrombolytic activity is achieved, but high effective dosages are required and anti-thrombotic and free radical scavenging activities are not verified
Solution Approach 1:
The patent combines three distinct functional components into a single conjugate molecule: (1) a tetrahydroisoquinoline compound with free radical scavenging activity, (2) a thrombolytic oligopeptide, and (3) a linking arm. This merging allows the drug to simultaneously exhibit thrombolytic, anti-thrombotic, and free radical scavenging activities at lower dosages, resolving the contradiction between achieving reliable thrombolytic activity and reducing the quantity of substance required.
Solution Approach 2:
The conjugate is designed to perform multiple functions simultaneously: thrombolytic activity through the oligopeptide component, anti-thrombotic activity through the tetrahydroisoquinoline component, and free radical scavenging through the same tetrahydroisoquinoline structure. This multi-functionality allows a single compound to address multiple aspects of thrombotic disease treatment, improving reliability while reducing the need for high dosages of single-function drugs.
2Reliability
If conventional thrombotic drugs are used, then thrombolytic effect is achieved, but efficacy is limited to treatment within 30 minutes from stroke onset
Solution Approach 1:
The conjugate provides continuous therapeutic action through multiple mechanisms: the thrombolytic oligopeptide actively dissolves existing clots, the tetrahowisoquinoline component prevents new thrombus formation through anti-thrombotic activity, and the free radical scavenging capability protects against oxidative damage throughout the treatment period. This continuous multi-faceted action extends the effective treatment window beyond the 30-minute limitation of conventional thrombolytics, allowing treatment to be effective up to 4 hours or more after stroke onset.
3Reliability
If thrombolytic activity is enhanced, then clot dissolution is improved, but systemic bleeding reactions may occur
Solution Approach 1:
The conjugate achieves local quality enhancement by combining thrombolytic, anti-thrombotic, and free radical scavenging functions in a single molecule that can be targeted to thrombotic sites. The thrombolytic oligopeptide component specifically acts on fibrin clots locally, while the tetrahowisoquinoline component provides local anti-thrombotic protection and free radical scavenging. This localized multi-functionality improves thrombolytic activity at the target site while reducing systemic exposure and minimizing bleeding reactions.
Data Source
AI summary
The present invention relates to a compound simultaneously having triple activities of thrombolysis, antithrombosis and free radical scavenging, as well as the preparation method, composition, and applications thereof. The compound is represented by the formula I shown below:wherein the definitions of T, Q, R1 and R2 are described herein. The compound of the present invention simultaneously has triple functions of thrombolysis, free radical scavenging and thrombus-targeting/antithrombosis. The present invention also relates to a pharmaceutical composition comprising the compound, and a preparation method and a nanostructure of the compound.