8-ヒドロキシ-5-ニトロキノリン 化学特性,用途語,生産方法
外観
うすい黄色～黄褐色、結晶性粉末～粉末
溶解性
アルカリ及び熱塩酸に易溶、アルコール、エーテルに微溶。
用途
有機合成原料、抗菌剤原料。
効能
抗菌薬, 尿路消毒薬
説明
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.
化学的特性
ochre-yellow to brownish crystalline powder
使用
antibacterial
定義
ChEBI: A monohydroxyquinoline in which the hydroxy group is positioned at C-8 with a nitro group trans to it at C-5.
世界保健機関（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drug was withdrawn in at least two countries.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.
8-ヒドロキシ-5-ニトロキノリン 上流と下流の製品情報
原材料
準備製品