Design and synthesis of bridged gamma-lactams as analogues of beta-lactam antibiotics |
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Authors: | Aszodi Jozsef Rowlands David A Mauvais Pascale Collette Pascal Bonnefoy Alain Lampilas Maxime |
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Institution: | Medicinal Chemistry, Aventis pharma, 102, route de Noisy, 93235 Romainville Cedex, France. |
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Abstract: | Anti-Bredt bridged bicyclo3.2.1] gamma-lactams were designed as inhibitors of penicillin binding proteins (PBPs). The compounds were prepared by a carbenoid insertion into a lactam N-H bond. Their weak antibacterial activity could either be explained by a poor chemical stability or by unfavorable steric interactions of the methylene bridge of the gamma-lactam with the targeted enzymes. |
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