Activity-directed expansion of a series of antibacterial agents. Issue 58 (15th June 2020)

• Record Type: Journal Article
• Authors: Leggott, Abbie; Clarke, Justin E.; Chow, Shiao; Warriner, Stuart L.; O'Neill, Alex J.; Nelson, Adam
• Is Part Of: Chemical communications. Volume 56:Issue 58(2020)
• Page Start: 8047
• Page End: 8050
• Publication Date: 2020-06-15
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc02361b
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Activity-directed synthesis harnessing 220 Pd-catalysed microscale reactions enabled expansion of a series of quinazolinone antibacterials. 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.