Three series of derived compounds of N, Aryl-N',Sulfamoyloxazolidin-2-ones were synthesized starting from chloro-sulfonylisocyanate (CSI) by carbomoylation, sulfamoylation and intramolecular cyclization reactions followed by methylation and heterocyclic reopening reactions. This later is based on a new hydrolysis method which uses a solid support, in order to obtain the correspondent amino-alcohols, which allowed isolating a new amino-alcohol ester. Measurements of the hydro-solubility by determination partition coefficient (log p) in water/octanol system were carried out by spectrophotometry. The antibacterial activities in vitro of some synthesized compounds were evaluated on a "Staphylococus aureus" strain in a Mûller-Hintone medium, showing good activity for some of them. All the synthesized compounds are characterized by IR, (1)H NMR and mass spectroscopy (ESI-MS).
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http://dx.doi.org/10.2174/157489107780832604 | DOI Listing |
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