Activity-directed expansion of a series of antibacterial agents.

Chemical Communications : Chem Comm
Abbie LeggottAdam Nelson

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.

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May 28, 2020·Chemistry : a European Journal·Adam I GreenAdam Nelson

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Citations

Jan 30, 2021·Accounts of Chemical Research·Mayland ChangShahriar Mobashery
Mar 20, 2021·ACS Medicinal Chemistry Letters·Kevin D DykstraShane W Krska
Dec 30, 2020·Chemical Reviews·Jed F Fisher, Shahriar Mobashery

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Methods Mentioned

BETA
NMR

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