Structure–Activity Relationships of Lactone Ring-Opened Analogs of the Antimalarial 1,2,4-Trioxane Artemisinin

• Main Authors: Gary H. Posner, David J. McGarvey, Chang Ho Oh, Nirbhay Kumar, Steven R. Meshnick, Wanida Asawamahasadka
• Other Authors: Johns Hopkins University
• Format: Article
• Published: 2018
• Subjects: Biochemistry, Genetics and Molecular Biology; Pharmacology, Toxicology and Pharmaceutics
• Online Access: https://repository.li.mahidol.ac.th/handle/123456789/17244
• Institution: Mahidol University

1,2,4-Trioxane benzylic ethers 8a–e were prepared as simplified, tricyclic versions of the clinically used tetracyclic antimalarial drug artemisinin (1). Five additional artemisinin analogs (9–11) were prepared. Neither water solubility (analogs 8e and 11b) nor chelating ability (analogs 9 and 10),...