Development of 6-Methanesulfonyl-8-nitrobenzothiazinone Based Antitubercular Agents.
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
14 Apr 2022
14 Apr 2022
Historique:
received:
19
11
2021
accepted:
04
03
2022
entrez:
22
4
2022
pubmed:
23
4
2022
medline:
23
4
2022
Statut:
epublish
Résumé
The 6-trifluoro substituted 8-nitrobenzothiazinones (BTZs) represent a novel type of antitubercular agents, and their high antimycobacterial activity is related to the inhibition of decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1), an enzyme essential for the biosynthesis of mycobacterial cell wall. While extraordinary whole-cell activity was reported for the clinically advanced compound PBTZ169, its poor aqueous solubility signals the potential low bioavailability. To ameliorate the BTZ physiochemical property, a series of 6-methanesulfonyl substituted compounds were designed and prepared, and their antitubercular activity and DprE1 inhibition ability were evaluated. Among these compounds, MsPBTZ169 and compounds
Identifiants
pubmed: 35450361
doi: 10.1021/acsmedchemlett.1c00652
pmc: PMC9014434
doi:
Types de publication
Journal Article
Langues
eng
Pagination
593-598Informations de copyright
© 2022 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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