Substituted Ethylene Diamines for Tuberculosis Treatment
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for tuberculosis, particularly those caused by drug-resistant strains, face challenges with compliance issues leading to the development of drug-resistant strains, and existing therapeutics like ethambutol have limitations in effectiveness and toxicity, necessitating new anti-tubercular agents with improved anti-mycobacterial activity.
Innovation Solution
Development of substituted ethylene diamine compounds with enhanced anti-tubercular activity, synthesized using solid polystyrene support and screened for Minimum Inhibition Concentration (MIC) and High-Throughput Screening (HTS) assays, which can be combined with antitubercular agents like rifampicin, isoniazid, pyrazinamide, and moxifloxacin to create effective therapeutic regimens.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing antitubercular agents like ethambutol are used, then treatment of tuberculosis can be provided, but effectiveness is limited and toxicity occurs
Solution Approach 1:
The patent modifies the chemical structure of ethambutol by substituting the hydroxyl groups with various functional groups (carboxylic acid, ester, amide, nitrile, etc.) to create analogues with improved pharmacological properties. This structural parameter change aims to enhance antitubercular effectiveness while reducing toxicity by altering how the drug interacts with biological systems.
Solution Approach 2:
The patent creates composite therapeutic regimens by combining substituted ethylene diamine compounds with existing antitubercular agents (rifampicin, isoniazid, pyrazinamide, moxifloxacin). This combination approach synergizes the properties of different compounds to achieve improved effectiveness while managing toxicity through complementary mechanisms of action.
2Adaptability or versatility
If current tuberculosis treatments are used, then existing therapeutic options are available, but compliance issues lead to development of drug-resistant strains
Solution Approach 1:
The patent divides the treatment approach into multiple components by creating a series of substituted ethylene diamine analogues that can be used in combination regimens. This segmentation allows for rotating or combining different agents to prevent resistance development, as multiple mechanisms of action are available rather than relying on a single drug.
Solution Approach 2:
The substituted ethylene diamine compounds are designed to serve multiple functions: they maintain antitubercular activity against drug-sensitive strains while also showing effectiveness against drug-resistant strains. This multi-functionality provides a versatile tool that can adapt to different resistance patterns and be used in various treatment scenarios.
3Reliability
If new substituted ethylene diamine compounds are developed, then anti-mycobacterial activity is enhanced, but synthesis and screening complexity increases
Solution Approach 1:
The synthesis approach segments the molecule into modular components: an ethylene diamine core structure with systematically varied substituents. This modular segmentation allows for efficient synthesis through combinatorial chemistry, where different functional groups are attached to the core using standardized reactions, reducing overall synthesis complexity despite the number of analogues being created.
Data Source
AI summary
Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.