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Activity-directed expansion of a series of antibacterial agents

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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.

Graphical abstract: Activity-directed expansion of a series of antibacterial agents

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Article information


Submitted
01 Apr 2020
Accepted
09 Jun 2020
First published
15 Jun 2020

This article is Open Access

Chem. Commun., 2020, Advance Article
Article type
Communication

Activity-directed expansion of a series of antibacterial agents

A. Leggott, J. E. Clarke, S. Chow, S. L. Warriner, A. J. O’Neill and A. Nelson, Chem. Commun., 2020, Advance Article , DOI: 10.1039/D0CC02361B

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