Unprecedented inhibition of resistant penicillin bindingproteins by bis-2-oxoazetidinylmacrocycles

Author:

Sliwa Aline12345,Dive Georges6785,Zervosen Astrid910115,Verlaine Olivier6785,Sauvage Eric6785,Marchand-Brynaert Jacqueline12345

Affiliation:

1. Institute of Condensed Matter and Nanosciences (IMCN)

2. Molecules, Solids and Reactivity (MOST)

3. Université Catholique de Louvain

4. Louvain-la-Neuve

5. Belgium

6. Centre d'ingénierie des Protéines (CIP)

7. Université de Liège

8. Sart-Tilman

9. Centre de Recherches du Cyclotron

10. B30, Université de Liège

11. Sart Tilman

Abstract

Bis-2-oxoazetidinyl macrocycles, obtained as unexpected products of RCM cyclizations, exhibit good activities against d,d-peptidase from Actinomadura R39 and revealed very promising activities against PBP2a from methicillin-resistant Staphylococcus aureus.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

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