Authors
Jean Gullion, Noel Pinaud, Lindita Lari, Luisa Ronga, Patrice Agnamey, Céline Damiani, Solène Savrimoutou, Elise Si Ahmed Charrier, Tshering Zangmo, Stéphane Moreau, Mathieu Marchivie, Sandra Albenque, Vanessa Desplat, Pascal Sonnet
Published in
Acta chimica Slovenica. Volume 73. Issue 3. Pages 713-723. Sep 11, 2026. Epub Sep 11, 2026.
Abstract
New pyrrolo[1,2-a]quinoxaline-2-carboxylic acid hydrazone derivatives were synthesized from nitroaniline using a multi-step pathway. Structure characterization of these novel substituted pyrrolo[1,2-a]quinoxaline-carboxylic acid hydrazones was achieved by using FT-IR, 1H NMR, 13C NMR, X-Ray and HRMS spectral analysis. These pyrroloquinoxaline hydrazone compounds were then evaluated in vitro for their potential on the human acute myeloid leukemia cell line MV4-11, in which (N'-pyridin-2-ylmethylene)pyrrolo[1,2-a]quinoxaline-2-carboxylic acid hydrazone 1a showed an IC50 value of 15.51 µM. Given the structural similarities between our hydrazone derivatives 1 and some recently published quinoline-type hydrazone compounds for antimalarial use, our compounds were also evaluated for their antimalarial activity. Among them, compound 1c demonstrated promising antiplasmodial activity, with an IC50 of 0.02 μM against the 3D7 strain of Plasmodium falciparum, exhibiting a selectivity index (SI) exceeding 5000 against this strain. Against the chloroquine-resistant Plasmodium falciparum W2 strain, hydrazone 1e emerged as the most potent and promising antimalarial candidate (IC50 = 0.03 mM), demonstrating a cytotoxicity to-antiprotozoal activity ratio exceeding 3333.
PMID:
42839563
Bibliographic data and abstract were imported from PubMed on 07 Oct 2026.
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