Fused Tricyclic Compounds for Broad-Spectrum Antimicrobial Activity

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Solution Overview

Problem

Current antibiotics are ineffective against antibiotic-resistant infections and lack efficacy against a wide range of microorganisms, including bacteria, viruses, and fungi, posing a significant threat to human health due to rising resistance and the need for new treatments.

Innovation Solution

Development of novel fused tricyclic compounds derived from plant-based chemistry, specifically tricyclic β-carboline adducts and dimer compounds, which inhibit microbial activity and treat microbial infections by reducing microbial titer and viability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If traditional antibiotics are used to treat infections, then they can address common bacterial infections, but they are ineffective against antibiotic-resistant strains and lack activity against viruses and fungi

Engineering Contradiction:

Improvespectrum of antimicrobial activityVSAvoidefficacy against resistant strains

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent develops fused tricyclic compounds that serve as universal antimicrobial agents effective against multiple types of microorganisms including bacteria, viruses, and fungi. The compounds of formula (I) and their derivatives demonstrate broad-spectrum activity, allowing a single agent to address diverse microbial threats that previously required multiple different antibiotics.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent modifies the chemical structure by introducing specific substituents at defined positions in the fused tricyclic core structure. By varying R1, R2, and R3 groups according to formula (I), the compounds achieve enhanced potency and activity against resistant strains while maintaining broad-spectrum coverage, representing a parameter change in molecular structure to overcome resistance.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If new antimicrobial compounds are developed to overcome resistance, then efficacy against resistant strains improves, but toxicity may increase

Engineering Contradiction:

Improveefficacy against resistant strainsVSAvoidtoxicity to host cells

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces specific functional groups and substituents at particular positions (R1, R2, R3) of the fused tricyclic core to optimize the balance between antimicrobial efficacy and host cell safety. These localized structural modifications enhance activity against resistant bacteria while maintaining selective toxicity, allowing the compound to distinguish between microbial and host cellular targets.

Inventive Principle:

Principle #3Local quality

Data Source

PatentUS20240002405A1Antimicrobial compounds, synthesis methods, and uses thereof

Publication Date: 2024.01.04 ANKH LIFE SCI LTD

AI summary

Fused tricyclic compounds and novel methods of synthesizing, using, and/or administering the same. Methods of inhibiting microbial activity and/or treating a microbial infection with fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds. The treatment of subjects suffering from a microbial infection comprises the step of administering to the subject one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds or a composition comprising one or more fused tricyclic compounds, bicyclic compounds, and other polycyclic compounds.