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Article Dans Une Revue Arabian Journal of Chemistry Année : 2017

New 3-substituted-2,1-benzisoxazoles: Synthesis and antimicrobial activities

Résumé

A new series of 3-substituted-2,1-benzisoxazoles (anthranils) were prepared by different methods and characterized by spectroscopic methods and mass spectrometry. These 2,1-benzisox-azoles were tested in vitro for their antiplasmodial activity on a chloroquine-resistant strain of Plasmodium falciparum (P.f.) (FcB1), and for antimicrobial activity against representative bacterial and fungal strains, as well as for cytotoxicity on MCF7 human breast cancer cells. Given the log P calc and selectivity index values (cytotoxicity/antiplasmodial activity ratio), the benzo[c]isoxazol-3-ylmethylene-phenyl-amine (11) (imino-benzisoxazole) was identified as the best hit against P.f. (FcB1), and the benzo[c]isoxazol-3-yl-phenyl-methanone (3) (3-acyl-2,1-benzisoxazole) against P.f. and the Geotrichum candidum fungal strain.
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Dates et versions

hal-02417861 , version 1 (18-12-2019)

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Paternité - Pas d'utilisation commerciale - Pas de modification

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Aida Chaker, Ennaji Najahi, Olivier Chatriant, Alexis Valentin, Nathan Téné, et al.. New 3-substituted-2,1-benzisoxazoles: Synthesis and antimicrobial activities. Arabian Journal of Chemistry, 2017, 10 (Supplement 2), pp.S2464-S2470. ⟨10.1016/j.arabjc.2013.09.011⟩. ⟨hal-02417861⟩
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