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Spiral molecules with antimalarial activities: A review
Jing Yang1, Yonggang Wang1, Wen Guan2
1Guangdong Engineering & Technology Research Center for Quality and Efficacy Reevaluation of Post-Market Traditional Chinese Medicine, Guangdong Key Laboratory of Plant Resources, School of Life Sciences, Sun Yat-sen University, Guangzhou, Guangdong, 510275, China.
European Journal of Medicinal Chemistry
|April 23, 2022
Summary
Drug resistance in malaria necessitates new treatments. This review highlights spiral structures as promising scaffolds for novel antimalarial drug development, offering new targets and overcoming resistance.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Drug Discovery
Background:
- Malaria remains a significant global health threat, particularly in tropical and subtropical areas.
- Existing antimalarial treatments face challenges due to widespread parasite resistance.
- Novel chemical compounds with new targets are crucial for effective malaria control.
Purpose of the Study:
- To review and summarize chemical compounds with antimalarial activities, focusing on spiral structures.
- To provide comprehensive information on structure-activity relationships, targets, resistance, and synthesis of antimalarial agents.
- To highlight the importance of spiral scaffolds in developing new drugs against malaria.
Main Methods:
- A literature review was conducted, covering publications from 1966 to 2021.
- Compounds were classified based on structural features, including spiro-peroxides, spiroindolones, and spirocyclohexadienones.
- Information on antimalarial activities, SAR, targets, resistance, and synthetic strategies was compiled.
Main Results:
- Various classes of spiral compounds exhibit significant antimalarial activity.
- Structure-activity relationship studies reveal key features for efficacy.
- The review details current development progress and synthetic approaches for these molecules.
Conclusions:
- Spiral structures represent a vital area for the development of novel antimalarial drugs.
- Understanding SAR and targets is essential for overcoming drug resistance.
- This review provides a foundation for future research in antimalarial drug discovery.
Keywords:
AntimalarialDrug resistanceSpiroSpiro-peroxidesSpirocyclohexadienonesSpiroindolonesStructure-activity relationshipSynthesis
