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Updated: May 22, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
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Third-generation analogues of Guttiferone A

David Hozain1, Kevin Cottet1, Yann Fromentin1

  • 1UMR CNRS 8038 CiTCoM, PNAS Team, Université Paris Cité, 75006 Paris, France.

Bioorganic & Medicinal Chemistry Letters
|March 14, 2025
PubMed
Summary

Third-generation guttiferone A derivatives show enhanced activity against Plasmodium falciparum and Trypanosoma brucei. Monodioxolane substitution in compound 3 significantly improved selectivity and potency.

Keywords:
Antiparasitic activityDioxolane derivativesGuttiferone aPlasmodium falciparumTrypanosoma brucei

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