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Structure-guided optimization of quinoline inhibitors of Plasmodium N-myristoyltransferase
Victor Goncalves1, James A Brannigan2, Alice Laporte1
1Department of Chemistry , Imperial College London , London SW7 2AZ , UK . Email: victor.goncalves@u-bourgogne.fr ;
Abstract:
The parasite Plasmodium vivax is the most widely distributed cause of recurring malaria. N-Myristoyltransferase (NMT), an enzyme that catalyses the covalent attachment of myristate to the N-terminal glycine of substrate proteins, has been described as a potential target for the treatment of this disease. Herein, we report the synthesis and the structure-guided optimization of a series of quinolines with balanced activity against both Plasmodium vivax and Plasmodium falciparum N-myristoyltransferase (NMT).
Insights
Researchers developed new quinoline compounds targeting the N-myristoyltransferase (NMT) enzyme. These compounds show promise for treating recurring malaria caused by Plasmodium vivax and Plasmodium falciparum.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Biochemistry
Background:
- Recurring malaria, primarily caused by Plasmodium vivax, poses a significant global health challenge.
- N-myristoyltransferase (NMT) is a crucial enzyme in parasite survival and a potential drug target.
- Existing treatments often face challenges with resistance and recurrence.
Purpose of the Study:
- To synthesize and optimize novel quinoline derivatives as inhibitors of Plasmodium NMT.
- To achieve balanced activity against both Plasmodium vivax and Plasmodium falciparum NMT.
- To explore structure-activity relationships for improved antimalarial drug development.
Main Methods:
- Structure-guided design and synthesis of quinoline compounds.
- Biochemical assays to evaluate NMT inhibitory activity.
- Testing against Plasmodium vivax and Plasmodium falciparum NMT enzymes.
Main Results:
- Successful synthesis of a novel series of quinoline derivatives.
- Demonstrated balanced inhibitory activity against both P. vivax and P. falciparum NMT.
- Identified key structural features contributing to potent NMT inhibition.
Conclusions:
- The developed quinoline compounds represent promising leads for novel antimalarial therapies.
- Targeting Plasmodium NMT with quinoline-based inhibitors offers a viable strategy against recurring malaria.
- Further optimization could lead to effective treatments for both P. vivax and P. falciparum malaria.
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