Identification of 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-N-phenylpropanamides as a novel class of potent DprE1 inhibitors

Benjamin C. Whitehurst, Robert J. Young, Glenn A. Burley, Monica Cacho, Pedro Torres, Laura Vela-Gonzalez del Peral

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8 Citations (Scopus)

Abstract

The identification of a novel series of DprE1 inhibitors based on a 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-N-phenylpropanamide scaffold is described herein. SAR exploration around the HTS hit 1 led to the identification of multiple analogues with potent DprE1 inhibition and good whole-cell antimycobacterial activity.
Original languageEnglish
Article number127192
JournalBioorganic and Medicinal Chemistry Letters
Volume30
Issue number12
Early online date13 Apr 2020
DOIs
Publication statusPublished - 15 Jun 2020

Keywords

  • Tuberculosis
  • DprE1
  • Inhibitor
  • 2,3-Dihydrobenzo[b][1,4]dioxin
  • Minimum inhibitory concentration

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