Related Experiment Video
Updated: Feb 6, 2026
07:02
Application of MassSQUIRM for Quantitative Measurements of Lysine Demethylase Activity
Published on: March 11, 2012
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Aryl-alkyl-lysines: small molecular membrane-active antiplasmodial agents
Chandradhish Ghosh1, Shweta Chaubey2, Utpal Tatu2
1Chemical biology and Medicinal Chemistry Laboratory , New Chemistry Unit , Jawaharlal Nehru Centre for Advanced Scientific Research (JNCASR) , Jakkur , Bengaluru 560064 , Karnataka , India .
Medchemcomm
|August 16, 2018
Summary
A new class of aryl-alkyl-lysine compounds shows promise as novel antimalarial drugs. These water-soluble, non-toxic compounds effectively target malaria parasites and improve survival in mouse models.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Drug Discovery
Background:
- Emerging resistance necessitates the development of new antimalarial drugs.
- Plasmodium falciparum remains a significant global health threat.
Purpose of the Study:
- To identify and characterize a new class of antimalarial compounds.
- To evaluate the efficacy and safety of aryl-alkyl-lysines against malaria.
Main Methods:
- Synthesis and screening of aryl-alkyl-lysine compounds.
- Assessment of antimalarial activity against Plasmodium falciparum ring stages.
- Evaluation in a murine model of malaria (Plasmodium berghei ANKA).
Main Results:
- A novel class of water-soluble, non-toxic aryl-alkyl-lysines demonstrated potent activity.
- The optimal compound disrupted parasite plasma membrane potential and digestive vacuole.
- Compounds increased survival by at least 5 days in a murine malaria model.
- No apparent toxicity was observed in mice at tested concentrations.
Conclusions:
- Aryl-alkyl-lysines represent a promising new class of antimalarial drug candidates.
- These compounds offer a potential solution to emerging drug resistance.
- Further research into aryl-alkyl-lysines is warranted for malaria treatment.
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