Kinetic parameters for the reaction of 1,2,4-trioxolanes and artemisinin with iron(II): New evidence for the source of antimalarial activity

Author(s)

Lopes, Nicolas S. ^[1] ; Ciscato, Luiz Francisco M. L. ^[1]

Affiliation

^[1] Univ Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre, SP - Brazil

• Document type: Journal article
• Source: CHEMICAL BIOLOGY & DRUG DESIGN; v. 91, n. 1, p. 328-331, JAN 2018.
• Web of Science Citations: 1

Abstract

The Fenton-like reductive cleavage of antimalarial peroxides like artemisinin by iron(II) species is a chemical reaction whose mechanistic pathway has not been yet fully understood; it is, however, known that there is considerable production of radical species centered at both the oxygen and carbon, which are important to the therapeutical effects of those compounds. This article reports kinetic data for the reaction of artemisinin and two model 1,2,4-trioxolanes with iron(II) species and also a mechanistic interpretation of this reductive cleavage from transition state thermodynamics. The suggestion of the presence of an enhancing specific factor inside the plasmodium is made. (AU)

• FAPESP's process: 12/02428-5 - Cyclic organic peroxides: synthesis and mechanism of reduction
• Grantee: Luiz Francisco Monteiro Leite Ciscato
• Support Opportunities: Regular Research Grants