Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

1,2,4-Trioxanes as potential antimalarial agents.

J A Kepler1, A Philip, Y W Lee

  • 1Research Triangle Institute, Research Triangle Park, North Carolina 27709.

Journal of Medicinal Chemistry
|April 1, 1988
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

A retrospective study on the outcomes of stapedotomy with vein graft interposition and vein graft surround techniques.

The Journal of laryngology and otology·2023
Same author

A cadaveric temporal bone study of the anatomical landmarks for middle turn cochleostomy.

The Journal of laryngology and otology·2023
Same author

The effects of N95 mask and face shield on speech perception among healthcare workers in the coronavirus disease 2019 pandemic scenario.

The Journal of laryngology and otology·2020
Same author

Sustained benefit of cognitive behaviour therapy for health anxiety in medical patients (CHAMP) over eight years: randomised controlled trial - CORRIGENDUM.

Psychological medicine·2020
Same author

Sustained benefit of cognitive behaviour therapy for health anxiety in medical patients (CHAMP) over 8 years: a randomised-controlled trial.

Psychological medicine·2020
Same author

Post-polypectomy surveillance colonoscopy: are we following the guidelines?

International journal of colorectal disease·2020
Same journal

Development of Indole-3-yl-methylene-thiobarbital Derivatives as Inhibitors of HDAC8 Enzyme Activity.

Journal of medicinal chemistry·2026
Same journal

Discovery of a Potent NAMPT-Targeting PROTAC for the Suppression of Triple-Negative Breast Cancer via Macrophage Reprogramming.

Journal of medicinal chemistry·2026
Same journal

3',4'-Isopropylidene-α-galactosylceramide Enables Multidose Th1 Adjuvanticity Despite Limited Serial Serum IFN-γ Responsiveness.

Journal of medicinal chemistry·2026
Same journal

A Bioorthogonally Cleavable <i>N</i>-Oxide Linker for Prodrug Design: Elucidating the Structure-Cyclization Kinetics Relationships for Controlled Drug Release.

Journal of medicinal chemistry·2026
Same journal

A Melatonin-Catechol Hybrid Molecule Prolongs Lifespan via Regulating ROS and Reprogramming Mitochondrial Metabolism.

Journal of medicinal chemistry·2026
Same journal

Discovery of SD-2301 as a Highly Potent and Selective PROTAC STAT3 Degrader Capable of Achieving Complete Tumor Regression with Single Administration.

Journal of medicinal chemistry·2026
See all related articles

Researchers synthesized 1,2,4-trioxanes as potential antimalarial drugs. Some compounds showed activity against Plasmodium falciparum, though less potent than qinghaosu.

Area of Science:

  • Medicinal Chemistry
  • Parasitology
  • Organic Synthesis

Background:

  • Malaria remains a significant global health challenge, necessitating new therapeutic agents.
  • Qinghaosu, a natural product, is a potent antimalarial but its complex structure poses synthetic challenges.
  • Development of simplified analogues of natural antimalarials is a key strategy in drug discovery.

Purpose of the Study:

  • To synthesize and evaluate novel 1,2,4-trioxane derivatives.
  • To identify simplified analogues of qinghaosu with antimalarial activity.
  • To assess the efficacy of these compounds against chloroquine-susceptible and resistant Plasmodium falciparum strains.

Main Methods:

  • Synthesis of a series of 1,2,4-trioxane compounds.
  • In vitro antimalarial activity assays using Plasmodium falciparum.

Related Experiment Videos

  • Determination of IC50 and IC20 values for compound efficacy.

    • Main Results:

    • Several 1,2,4-trioxane derivatives were successfully synthesized.
    • Compounds 3b and 12 demonstrated notable in vitro antimalarial activity.
    • Compound 3b showed IC20 values of 96 and 39 ng/mL, while compound 12 had IC50 values of 24 and 99 ng/mL against the tested strains.
    • Activity was generally lower compared to the reference drug qinghaosu.

    Conclusions:

    • 1,2,4-Trioxanes represent a promising scaffold for antimalarial drug development.
    • Simplified analogues can retain significant antimalarial properties.
    • Further optimization may lead to more potent antimalarial agents.