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 language | English |
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Article number | 127192 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 30 |
Issue number | 12 |
Early online date | 13 Apr 2020 |
DOIs | |
Publication status | Published - 15 Jun 2020 |
Keywords
- Tuberculosis
- DprE1
- Inhibitor
- 2,3-Dihydrobenzo[b][1,4]dioxin
- Minimum inhibitory concentration