Quinoline Anthelmintic Compounds for Resistant Heartworm Treatment
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Solution Overview
Problem
The emergence of resistant worm populations against existing anthelmintic compounds poses a significant challenge in effectively treating helminth infections in mammals, particularly in pets like dogs and cats, with heartworm disease being a severe and often fatal condition.
Innovation Solution
Development of new anthelmintic compounds, specifically those with a quinoline structure, that target parasitic helminths such as Dirofilaria immitis, offering compatibility with standard antiparasitic treatments and minimal side effects, and can be administered orally or topically.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing anthelmintic compounds are used to treat helminth infections, then treatment effectiveness is reduced, but worm populations develop resistance
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of anthelmintic compounds through various substituents (R1-R6, R8-R12) on the quinoline core. This structural variation creates new compounds with potentially different biological activities that can overcome existing worm resistance while maintaining treatment effectiveness.
Solution Approach 2:
The invention uses composite molecular structures combining a quinoline core with diverse substituent groups (halogens, alkyl chains, heterocyclic rings, carbonyl groups). These composite structures aim to achieve synergistic effects that enhance anthelmintic activity while reducing resistance development.
2Object-affected harmful factors
If new anthelmintic compounds with quinoline structure are developed, then resistance issues are reduced, but treatment compatibility and side effect profile must be optimized
Solution Approach 1:
The patent systematically varies chemical parameters (substituent types, positions, and combinations) to optimize the balance between anthelmintic efficacy and host compatibility. By adjusting molecular properties, the compounds aim to achieve selective toxicity against worms while minimizing side effects in mammalian hosts.
3Ease of operation
If anthelmintic compounds are administered orally or topically, then treatment ease is improved, but systemic side effects may increase
Solution Approach 1:
The chemical structure parameters of the quinoline compounds are optimized to achieve appropriate pharmacokinetic properties. By adjusting molecular weight, lipophilicity, and functional groups, the compounds aim to achieve effective absorption through oral or topical routes while limiting systemic distribution and reducing potential side effects.
Data Source
AI summary
The present invention relates to new anthelmintic compounds. These compounds can for example be used in the treatment of the kind of worm disease caused by helminths such as Dirofilaria, in particular Dirofilaria immitis.