Identification of 2-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-N-phenylpropanamides as a novel class of potent DprE1 inhibitors.
Alcohol Oxidoreductases
/ antagonists & inhibitors
Antitubercular Agents
/ chemical synthesis
Bacterial Proteins
/ antagonists & inhibitors
Dose-Response Relationship, Drug
Enzyme Inhibitors
/ chemical synthesis
Microbial Sensitivity Tests
Molecular Structure
Mycobacterium tuberculosis
/ drug effects
Structure-Activity Relationship
2,3-Dihydrobenzo[b][1,4]dioxin
DprE1
Inhibitor
Minimum inhibitory concentration
Tuberculosis
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 06 2020
15 06 2020
Historique:
received:
28
01
2020
revised:
05
04
2020
accepted:
11
04
2020
pubmed:
22
4
2020
medline:
13
5
2021
entrez:
22
4
2020
Statut:
ppublish
Résumé
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.
Identifiants
pubmed: 32312582
pii: S0960-894X(20)30291-2
doi: 10.1016/j.bmcl.2020.127192
pii:
doi:
Substances chimiques
Antitubercular Agents
0
Bacterial Proteins
0
Enzyme Inhibitors
0
Alcohol Oxidoreductases
EC 1.1.-
DprE1 protein, Mycobacterium tuberculosis
EC 1.1.-
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
127192Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.