Antimalarial Agents: Design and Mechanism of Action

The Design and Synthesis of Antimalarial Agents is a comprehensive, yet accessible, guide for those involved in the design, development and administration of antimalarial drugs. The book's aim is to support medicinal chemists in their search for improved and novel antimalarial drugs, providing practical guidance on current developments and highlighting promising leads. Beginning with a focus on the biological aspects of malaria, the book discusses the lifecycle of the parasite responsible for malaria, the problem of resistance, combinational therapy, genetic mapping of the parasite’s genome, established drug targets, and potential drug targets for the future.

In addition, it covers the medicinal chemistry of antimalarial agents in detail, with a focus on the design of antimalarial drugs supported by a review of the drug categories that have reached the market, as well as those in the pipeline. Finally, the synthesis of different classes of antimalarial agents is reviewed, including a discussion on chemical and process development.

Consolidates, for the first time, current developments in the discovery, design and synthesis of antimalarial drugs Presents content in a style that is both thorough and engaging, supporting and encouraging students and researchers from interdisciplinary backgrounds Highlights which drug targets are currently considered to be the most promising for future therapies and the classes of compounds being studied and perfected

1. History of malaria and its treatment 2. Knowing one's enemy: the Plasmodium parasite 3. The cinchona alkaloids and the aminoquinolines 4. Artemisinin and artemisinin-related agents 5. Agents acting on pyrimidine metabolism 6. Antimalarial agents acting on hemoglobin degradation 7. Plasmepsins as targets for antimalarial agents 8. Falcipains as drug targets in antimalarial therapy 9. Drug targets in the apicoplast 10. Drugs targeting mitochondrial functions 11. The Plasmodium falciparum proteasome as a drug target 12. Transferases and their inhibition 13. Kinases and kinase inhibitors 14. Miscellaneous agents of clinical interest 15. Inhibitors of purine and pyrimidine pathways 16. Miscellaneous targets