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Synthesis and antibacterial activity of racemic paecilocin A and its derivatives against methicillin-sensitive and -resistant Staphylococcus aureus

Abstract : A total synthesis in four steps of racemic paecilocin A, a natural marine phthalide is reported. The synthetic pathway includes an iodine-magnesium exchange followed by a condensation on an aldehyde and represents a sufficiently flexible approach to allow the synthesis of twelve analogs. The synthesized compounds were investigated for their antibacterial activity against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant strain (MRSA). Three analogs were found to have similar or better antibacterial activity than the natural compound on MRSA. (C) 2021 Elsevier Ltd. All rights reserved.
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https://hal.inrae.fr/hal-03205212
Contributor : Nathalie Katy Chanteloup <>
Submitted on : Thursday, April 22, 2021 - 10:31:04 AM
Last modification on : Thursday, May 6, 2021 - 2:21:49 PM

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Walaa Ibraheem, Quentin Wils, Emilie Camiade, Elhadi Ahmed, Jérôme Thibonnet, et al.. Synthesis and antibacterial activity of racemic paecilocin A and its derivatives against methicillin-sensitive and -resistant Staphylococcus aureus. Tetrahedron Letters, Elsevier, 2021, 67, 4 p. ⟨10.1016/j.tetlet.2021.152888⟩. ⟨hal-03205212⟩

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