Bioorganic & Medicinal Chemistry 2015-02-01

Non-transpeptidase binding arylthioether β-lactams active against Mycobacterium tuberculosis and Moraxella catarrhalis.

Tim N Beck, Dina Lloyd, Rostislav Kuskovsky, Jeanette Minah, Kriti Arora, Balbina J Plotkin, Jacalyn M Green, Helena I Boshoff, Clifton Barry, Jeffrey Deschamps, Monika I Konaklieva

Index: Bioorg. Med. Chem. 23(3) , 632-47, (2015)

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Abstract

The prevalence of drug resistance in both clinical and community settings as a consequence of alterations of biosynthetic pathways, enzymes or cell wall architecture is a persistent threat to human health. We have designed, synthesized, and tested a novel class of non-transpeptidase, β-lactamase resistant monocyclic β-lactams that carry an arylthio group at C4. These thioethers exhibit inhibitory and cidal activity against serine β-lactamase producing Mycobacterium tuberculosis wild type strain (Mtb) and multiple (n=8) β-lactamase producing Moraxella catarrhalis clinical isolates. Copyright © 2014 Elsevier Ltd. All rights reserved.