Issue 58, 2020

Activity-directed expansion of a series of antibacterial agents

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

Supplementary files

Article information

Article type
Communication
Submitted
01 Apr 2020
Accepted
09 Jun 2020
First published
15 Jun 2020
This article is Open Access
Creative Commons BY license

Chem. Commun., 2020,56, 8047-8050

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, 56, 8047 DOI: 10.1039/D0CC02361B

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements