Affinity-Based Screen for Inhibitors of Bacterial Transglycosylase

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Date: Feb. 28, 2018
From: Journal of the American Chemical Society(Vol. 140, Issue 8)
Publisher: American Chemical Society
Document Type: Report
Length: 89 words

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Abstract :

The article reports an affinity-based ligand screen method using penicillin-binding proteins immobilized on beads to selectively isolate the binders from complex natural products. In combination with mass spectrometry and assays with moenomycin A and salicylanilide analogues (1u10) as reference inhibitors, four potent antibacterials confirmed to be benastatin derivatives (11u13) and albofungin (14), are isolated. Compounds 11 and 14 are effective antibiotics against a broad-spectrum of Gram-positive and Gram-negative bacteria, including Acinetobacter baumannii, Clostridium difficile, Staphylococcus aureus, and drug-resistant strains with minimum inhibitory concentrations in the submicromolar to nanomolar range.

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Gale Document Number: GALE|A536080388