Non-transpeptidase binding arylthioether β-lactams active against Mycobacterium tuberculosis and Moraxella catarrhalis. Issue 3 (1st February 2015)

• Record Type: Journal Article
• Authors: Beck, Tim N.; Lloyd, Dina; Kuskovsky, Rostislav; Minah, Jeanette; Arora, Kriti; Plotkin, Balbina J.; Green, Jacalyn M.; Boshoff, Helena I.; Barry, Clifton; Deschamps, Jeffrey; Konaklieva, Monika I.
• Is Part Of: Bioorganic & medicinal chemistry. Volume 23:Issue 3(2015)
• Page Start: 632
• Page End: 647
• Publication Date: 2015-02-01
• Subjects: Mycobacterium tuberculosis -- Moraxella catarrhalis -- β-Lactams -- Antimicrobial resistance; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2014.11.025
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: 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.