N-thiolated 2-oxazolidone antibiotics

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 413/12 (2006.01) A61K 31/421 (2006.01) C07D 263/04 (2006.01)

Patent

CA 2607660

This invention describes the discovery and synthesis of N-thiolated 2- oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2- oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.

Cette invention décrit la découverte et la synthèse de 2-oxazolidinones N-thiolatées comme nouvelle classe d~agents anti-bactériens. Ces composés peuvent être synthétisés à partir de 2-oxazolidinones par N-déprotection et N-sulfénylation. On a trouvé que ces nouvelles substances montrent une activité anti-bactérienne puissante, y compris des propriétés bactériostatiques contre Staphylococcus spp., y compris Staphylococcus aureus résistant à la méthicilline (MRSA), et Bacillus spp., y compris Bacillus anthracis.

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