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Chemical and Antiplasmodial Investigations on <i>Carapa</i>-Derived Gedunin Derivatives and Semisynthetic 6- and 7‑Substituted Gedunin Analogues from the Brazilian Amazon.


ABSTRACT: The aim of this work was to explore structure-antiplasmodial activity relationships among 6- and 7-acyloxy and hydroxy substituted gedunin derivatives. 7-Deacetyl-7-oxogedunin (cedrolide, 1) and 6α-acetoxygedunin (12)known antiplasmodial limonoids from the seeds of Carapa guianensis Aublet (Meliaceae)were targeted for isolation at scale and used as starting materials for the preparation of a small, semisynthetic compound library that included gedunin (4), 7α- or 7β-acyloxy substituted 7-deacetylgedunins (5-9), and 6α-acyloxy substituted 7-deacetylgedunin derivatives (13-15). The concentrations of these compounds that inhibit 50% of the in vitro growth (IC50) of the multidrug-resistant K1 strain of the human malaria parasi

SUBMITTER: Barbosa Pereira T 

PROVIDER: S-EPMC12529149 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature