Synthesis, antibacterial and cytotoxic evaluation of cytosporone E and analogs

Walaa Ibraheem; Capucine Chaar; Emilie Camiade; Virginie Hervé; Delphine Fouquenet; Anne-Emmanuelle Roux; Mustapha Si-Tahar; Elhadi Ahmed; Jérôme Thibonnet; Emilie Thiery; Julien Petrignet

doi:10.1016/j.molstruc.2021.132135

Journal articles

Synthesis, antibacterial and cytotoxic evaluation of cytosporone E and analogs

Walaa Ibraheem ^{1, 2} Capucine Chaar ^{1, 3} Emilie Camiade ⁴ Virginie Hervé ³ Delphine Fouquenet ³ Anne-Emmanuelle Roux ⁴ Mustapha Si-Tahar ³ Elhadi Ahmed ² Jérôme Thibonnet ¹ Emilie Thiery ¹ Julien Petrignet ^{1, *}

* Corresponding author

1 SIMBA - Synthèse et isolement de molécules bio-actives EA 7502

2 University of Gezira

3 CEPR - Centre d’Etude des Pathologies Respiratoires (CEPR), UMR 1100

4 UMR ISP - Infectiologie et Santé Publique

Abstract : The history of antibacterial discovery has revealed that natural products, especially secondary metabolites, represent privileged chemical matters for the antibacterial discovery. Among these metabolites, several natural phthalides exhibit interesting antibacterial activities, such as cytosporone E isolated from endophyte ascomycetes Diaporthe and Cytospora sp. We describe herein the synthesis and the pharmacomulations on the positions 3, 4 and 6 of cytosporone E, then the in vitro antibacterial evaluation of these compounds against Staphylococcus aureus including resistant strains, Escherichia coli and Pseudomonas aeruginosa. The evaluation of the cytotoxicity of the most active compounds against human bronchial epithelial cells was performed in order to check their safety.

Keywords : natural phthalide pharmacomodulations antibacterial activity cytotoxicity

Document type :

Journal articles

Domain :

Chemical Sciences / Organic chemistry

Life Sciences [q-bio] / Microbiology and Parasitology / Bacteriology

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https://hal.inrae.fr/hal-03509478
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Submitted on : Tuesday, January 4, 2022 - 10:56:37 AM
Last modification on : Tuesday, May 17, 2022 - 10:58:38 AM

Synthesis, antibacterial and cytotoxic evaluation of cytosporone E and analogs

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