Acylphosphates and acylphosphonates as .beta.-lactamase and...

C - Chemistry – Metallurgy – 07 – F

Patent

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C07F 9/40 (2006.01) A61K 31/66 (2006.01) C07F 9/09 (2006.01) C07F 9/6571 (2006.01) C07F 9/6574 (2006.01)

Patent

CA 2315821

The invention provides novel .beta.-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic .beta.- lactamase inhibitors presently available, and which do not possess .beta.- lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as .beta.-lactamase inhibitors and as antibiotics.

L'invention concerne de nouveaux inhibiteurs de beta -lactamases, qui ne sont pas structurellement liés au produit naturel et aux inhibiteurs de beta -lactamases semi-synthétiques actuellement disponibles, et qui ne possèdent pas un pharmacophore des beta -lactamases. Ces nouveaux inhibiteurs sont entièrement synthétiques et permettent ainsi d'avoir facilement accès à une grande variété d'analogues liés structurellement. Certains de ces nouveaux inhibiteurs se lient également à des DD-peptidases bactériennes, agissant ainsi potentiellement comme inhibiteurs de beta -lactamases et comme antibiotiques.

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