Oxadiazole-pyridine quaternary ammonium salt-containing side-chain pleuromutilin derivative with drug-resistant bacterium resisting activity and preparation method and application of oxadiazole-pyridine quaternary ammonium salt-containing side-chain pleuromutilin derivative

The invention discloses a pleuromutilin derivative with drug-resistant bacterium resisting activity and an oxadiazole-pyridine quaternary ammonium salt side chain as well as a preparation method and application of the pleuromutilin derivative, and belongs to the technical field of medicinal chemistr...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: WAN JIA, HAN JUNJIE, LIANG CHENGYUAN, XIN LIANG, WU KANGXIONG, PENG ZHAORUI, KONG CHUNCHUN, ZHANG SHAOJUN
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention discloses a pleuromutilin derivative with drug-resistant bacterium resisting activity and an oxadiazole-pyridine quaternary ammonium salt side chain as well as a preparation method and application of the pleuromutilin derivative, and belongs to the technical field of medicinal chemistry. The pleuromutilin derivative containing the oxadiazole-pyridine quaternary ammonium salt side chain is simply and efficiently prepared through the three-step reaction, the reaction raw materials are cheap and easy to obtain, the reaction conditions are mild, the product yield is high, and the method is suitable for industrial production. In-vitro antibacterial experiments on gram-positive bacteria such as methicillin-resistant staphylococcus aureus and gram-negative bacteria such as escherichia coli show that the pleuromutilin derivative synthesized by the invention has relatively strong antibacterial activity. In-vitro cytotoxicity experiments on HepG2, HEK293 and A549 cells show that the pleuromutilin derivati