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Bioorg Med Chem Lett. 2007 Sep 15;17(18):5171-4. Epub 2007 Jul 5.

A minimalistic approach to identify substrate binding features in B1 Metallo-beta-lactamases.

Author information

1
Instituto de Química Orgánica de Síntesis (UNR-CONICET), Suipacha 570, S2002LRK Rosario, Argentina.

Abstract

The 2-oxoazetidinylacetate sodium salt was synthesized as a model of a minimal beta-lactam drug. This compound and the monobactam aztreonam were assayed as substrates of the Metallo-beta-lactamase BcII. None of them was hydrolyzed by the enzyme. While the azetidinone was not able to bind BcII, aztreonam was shown to bind in a nonproductive mode. These results provide an explanation for the unability of Metallo-beta-lactamases to inactive monobactams and give some clues for inhibitor design.

PMID:
17644332
DOI:
10.1016/j.bmcl.2007.06.089
[Indexed for MEDLINE]

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