Nitroxolin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R20/21/22:Gesundheitssch?dlich beim Einatmen,Verschlucken und Berührung mit der Haut.
S-S?tze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn m?glich, dieses Etikett vorzeigen).
Beschreibung
Nitroxoline is an 8-hydroxyquinoline that has diverse biological activities, including antibacterial, antiproliferative, and bromodomain interaction-inhibiting properties. Nitroxoline is active against the bacteria
E. coli,
S. aureus,
E. faecalis,
K. pneumoniae, and
P. mirabilis in vitro (MIC
90s = 4, 4, 8, 8, and 8 mg/L, respectively). It also inhibits biofilm formation of certain strains of multidrug-resistant (MDR)
A. baumannii and
P. aeruginosa, as well as methicillin-resistant
S. aureus (MRSA) and
S. epidermidis (MRSE) with minimum biofilm eradication concentration (MBEC) values of 46.9, 1,500, 188, and 125 μM, respectively. Nitroxoline inhibits the growth of human U87 and U251 glioma, A549 lung, and PC3 prostate cancer cells (IC
50s = 50, 6, 38, and 23 μg/ml, respectively).
In vivo, it reduces tumor growth in a PTEN- and KRAS-driven glioma mouse model when administered at a dose of 80 mg/kg per day. Nitroxoline also inhibits the interaction between the first bromodomain of bromodomain-containing protein 4 (BRD4) with acetylated histone H4 with an IC
50 value of 0.98 μM.
Chemische Eigenschaften
ochre-yellow to brownish crystalline powder
Verwenden
antibacterial
Definition
ChEBI: A monohydroxyquinoline in which the hydroxy group is positioned at C-8 with a nitro group trans to it at C-5.
Weltgesundheitsorganisation (WHO)
Nitroxoline, a urinary antiseptic, was introduced in the mid-1960s.
By the early 1970s long-term animal studies revealed the development of cataracts
in rats and, although no serious adverse effects had been reported in man, the
drug was withdrawn in at least two countries. Preparations containing nitroxoline remain widely available.
Nitroxolin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte