Rapid synthesis of sulfone derivatives as potential anti-infectious agents.
An original one-pot microwave reaction was developed for the synthesis of sulfone derivatives as new potent antimicrobial agents. This eco-friendly methodology conducted in 30min led to desired products with good yields. The sulfones (4a and 4b) were obtained via the reaction of 3a with the corresponding halo-derivatives in the presence of sodium hydride. All compounds were tested for their antibacterial and antifungal activities against four bacterial strains (two gram positive, and two gram negative ones) and two yeasts. The disk diffusion method has shown an interesting antibacterial activity for seven compounds (3b-g and 4b) against Staphylococcus aureus. Among these seven compounds, five derivatives (3b-e and 3g) showed activity against Candida tropicalis.
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Laboratoire de Chimie Organique Pharmaceutique, Université de la Méditerranée, UMR CNRS 6517, Faculté de Pharmacie, 27 boulevard Jean Moulin, 13385 Marseille Cedex 05, France.
Laget
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Carle
A Ortiz
AO
Gellis
A
A
Vanelle
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P
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000890:Anti-Infective Agents; D013450:Sulfones