Antibiotic natural product hunanamycin A: Lead identification towards anti-Salmonella agents
Design and synthesis of library of compounds around the antibiotic natural product hunanamycin A scaffold and their biological evaluation are disclosed here. These efforts resulted in identification of a lead compound 36, which is a structurally simplified analogue of original hunanamycin A with imp...
Gespeichert in:
Veröffentlicht in: | European journal of medicinal chemistry 2022-06, Vol.236, p.114245-114245, Article 114245 |
---|---|
Hauptverfasser: | , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | Design and synthesis of library of compounds around the antibiotic natural product hunanamycin A scaffold and their biological evaluation are disclosed here. These efforts resulted in identification of a lead compound 36, which is a structurally simplified analogue of original hunanamycin A with impressive activity against Salmonella enterica and possesses other druggable properties. In addition, no acute oral toxicity was observed for compound 36 in Swiss albino mice dosed up to 2 g/kg. It has the potential to be developed for the treatment of food infections caused by Salmonella.
[Display omitted]
•Designed and synthesized >70 analogues of antibiotic natural product hunanamycin A and screened against Salmonella enterica.•Identified of four inhibitors 27, 40, 36, and 62 more potent than HA and established valuable SARs.•Lead compound 36, a simplified analogue possesses impressive activity against S. enterica with decent in vitro ADME profile.•No acute oral toxicity was observed for compound 36 in Swiss albino mice dosed up to 2 g/Kg. |
---|---|
ISSN: | 0223-5234 1768-3254 |
DOI: | 10.1016/j.ejmech.2022.114245 |