Identification of 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-N-phenylpropanamides as a novel class of potent DprE1 inhibitors
Whitehurst BC, Young RJ, Burley GA, Cacho M, Torres P, Vela-Gonzalez Del Peral L
Bioorganic & medicinal chemistry letters · 2020-04
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.
MeSH terms
- Mycobacterium tuberculosis
- Alcohol Oxidoreductases
- Bacterial Proteins
- Enzyme Inhibitors
- Antitubercular Agents
- Microbial Sensitivity Tests
- Molecular Structure
- Structure-Activity Relationship
- Dose-Response Relationship, Drug