Activity-directed expansion of a series of antibacterial agents

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Leggott, Abbie and Clarke, Justin E. and Chow, Shiao and Warriner, Stuart L. and O'Neill, Alex J. and Nelson, Adam (2020) Activity-directed expansion of a series of antibacterial agents. Chemical Communications, 56 (58). pp. 8047-8050. ISSN 1359-7345 (https://doi.org/10.1039/D0CC02361B)

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Abstract

The feasibility of using activity-directed synthesis to drive antibacterial discovery was investigated. An array of 220 Pd-catalysed microscale reactions was executed, and the crude product mixtures were evaluated for activity against Staphylococcus aureus. Scale-up of the hit reactions, purification and evaluation, enabled expansion of a class of antibacterial quinazolinones. The novel antibacterials had MICs from 0.016 μg mL−1 (i.e. 38 nM) to 2–4 μg mL−1 against S. aureus ATCC29213.

ORCID iDs

Leggott, Abbie, Clarke, Justin E., Chow, Shiao ORCID logoORCID: https://orcid.org/0000-0002-3600-0497, Warriner, Stuart L., O'Neill, Alex J. and Nelson, Adam;
CORE (COnnecting REpositories)