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

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, ?-lactamase resistant monocyclic ?-lactams that carry an arylthio group at C4. These thioethers exhibit inhibitory and cidal activity against serine ?-lactamase producing Mycobacterium tuberculosis wild type strain (Mtb) and multiple (n=8) ?-lactamase producing Moraxella catarrhalis clinical isolates.

SUBMITTER: Beck TN

PROVIDER: S-EPMC6415315 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature

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

Beck Tim N TN Lloyd Dina D Kuskovsky Rostislav R Minah Jeanette J Arora Kriti K Plotkin Balbina J BJ Green Jacalyn M JM Boshoff Helena I HI Barry Clifton C Deschamps Jeffrey J Konaklieva Monika I MI

Bioorganic & medicinal chemistry 20141212 3

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 ...[more]

PMID: 25549898

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