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Novel hybrid 1,4-naphthoquinone-endoperoxide antimalarial hits: synthesis, stereoisomeric separation, and biological evaluation

delete2026-05-09
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OA
AI
A
Alexandre Benech
S
Sébastien Hutter
N
Nicolas Vanthuyne
O
Omar Khoumeri
C
Christophe Curti *
P
Patrice Vanelle *
T
Thierry Terme
N
Nadine Azas
DOI:10.1016/j.ejmech.2026.118926delete
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Abstract

Abstract

En 中文
• First naphthoquinone-endoperoxide dual-pharmacophore antimalarial hybrids • Mn(III)-mediated peroxycyclization enabled access to stereoisomeric series • Full stereoisomer resolution was achieved by preparative chiral HPLC • Stereochemistry significantly influenced potency (3-fold) and selectivity (9-fold) • Lead exhibited IC50 0.49 μM against MDR P. falciparum W2 with SI >250 on CHO
Keywords:
naphthoquinone
endoperoxide
antimalarial
stereoisomers
hybrid compounds
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Journal

European Journal of Medicinal Chemistry cover
European Journal of Medicinal Chemistry
IF:
5.9
Papers:
1.7W
Citations:
6.0W

Organization

C
cnrs and centrale med
Scholars:
1
Papers: 1
Citations: 0
P
pharmacie
Scholars:
29
Papers: 14
Citations: 0
R
ritmes
Scholars:
9
Papers: 6
Citations: 0
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