Dispiro- 1,2,4,5-tetraoxanes: A New Class of Antimalarial Peroxides

Authors

Jonathan L. Vennerstrom, University of Nebraska Medical CenterFollow
Hong-Ning Fu, University of Nebraska Medical Center
Walter Reed Army Institute of Research
Arba L. Ager Jr., University of Miami
James K. Wood, University of Nebraska at OmahaFollow
Walter Reed Army Institute of Research
Walter Reed Army Institute of Research
Walter Reed Army Institute of Research

Document Type

Article

Publication Date

8-1992

Publication Title

Journal of Medicinal Chemistry

Volume

35

Issue

16

First Page

3023

Last Page

3027

Abstract

Dispiro-l,2,4,5tetraoxanes2 -4 were synthesized as potential peroxide a n t h a l a* d drugs. They had curative activity against Plasmodium berghei in vivo at single doses of 320 and 640 mg/kg which confirms earlier unpublished data Moreover, artemisinin (1) and 4 had equivalent ED”s against P. berghei in vivo in the multiple-dose Thompson tat; neither showed any evidence of acute toxicity at total doses of more than 12 g/kg. Dispiro-l,2,4,5-tetraoxane 4 had IC₅₀’s comparable to those of 1 against Plasmodium falciparum clones in vitro. These results confirm the potential of dispiro-l,2,4,5-tetraoxanes as a new class of inexpensive peroxide antimalarial drugs.

Comments

Copyright © 1992, American Chemical Society.

Recommended Citation

Vennerstrom, Jonathan L.; Fu, Hong-Ning; Walter Reed Army Institute of Research; Ager, Arba L. Jr.; Wood, James K.; Walter Reed Army Institute of Research; Walter Reed Army Institute of Research; and Walter Reed Army Institute of Research, "Dispiro- 1,2,4,5-tetraoxanes: A New Class of Antimalarial Peroxides" (1992). Chemistry Faculty Publications. 19.
https://digitalcommons.unomaha.edu/chemfacpub/19