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ChemicalBook Optimization Suppliers |
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| 化学名: | ナジフロキサシン | | 英語化学名: | Nadifloxacin | | 别名: | NDFX;Nadifiloxacin;NadifloxacinAPI;7-fluoro-8-(4-hydroxypiperidin-1-yl)-12-Methyl-4-oxo-1-azatricyclo[7.3.1.0^{5,13}]trideca-2,5(13),6,8-tetraene-3-carboxylic acid;9-Fluoro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-6,7-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-2-carboxylic acid;NADIFLOXACIN;9-Fluoro-6,7-dihydro-8-(4-hydroxy-1-piperidinyl)-5-methyl-1-oxo-1H,5H-benzo[ij]quinolizine-2-carboxylic Acid;Acuati | | CAS番号: | 124858-35-1 | | 分子式: | C19H21FN2O4 | | 分子量: | 360.38 | | EINECS: | 638-863-6 | | カテゴリ情報: | ACUATIM;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 124858-35-1.mol |  |
| 融点 | 245-2470C (dec) | | 沸点 | 624.9±55.0 °C(Predicted) | | 比重(密度) | 1.46±0.1 g/cm3(Predicted) | | 貯蔵温度 | Sealed in dry,Store in freezer, under -20°C | | 溶解性 | DMSO (Slightly), Methanol (Sparingly, Heated) | | 外見 | White to yellow crystalline solid. | | 酸解離定数(Pka) | 5.55±0.40(Predicted) | | 色 | White to Off-White | | Merck | 14,6345 | | InChI | InChI=1S/C19H21FN2O4/c1-10-2-3-12-16-13(18(24)14(19(25)26)9-22(10)16)8-15(20)17(12)21-6-4-11(23)5-7-21/h8-11,23H,2-7H2,1H3,(H,25,26) | | InChIKey | JYJTVFIEFKZWCJ-UHFFFAOYSA-N | | SMILES | C12=CC(F)=C(N3CCC(O)CC3)C3=C1N(C(C)CC3)C=C(C(O)=O)C2=O | | CAS データベース | 124858-35-1(CAS DataBase Reference) |
| HSコード | 2933.99.7500 | | 毒性 | LD50 male, female mice and rats (mg/kg): 376.5, 420.6, 225.7, 240.5 i.v. (Hashimoto) |
| | ナジフロキサシン Usage And Synthesis |
| 外観 | 白色～黄色、結晶～粉末 | | 溶解性 | 水酸化ナトリウム溶液に溶ける。 | | 用途 | ニューキノロン系抗菌剤です。
DNA ジャイレースを阻害します。抗菌スペ
クトルは非常に広く、アクネ菌及び表皮ブド
ウ菌球菌を含むグラム陽性菌、グラム陰性菌
に対して、強い抗菌作用を示します。MRSA、
キノロン耐性 MRSA に対しても抗菌作用を示
します。 | | 効能 | 抗菌薬, 核酸合成阻害薬 | | 商品名 | アクアチム (大塚製薬); アクアチム (大塚製薬); アクアチム (大塚製薬) | | 説明 | Nadifloxacin, one of the three new fluoroquinolone antibiotics launched in 1993 is
indicated for topical treatment of acne vulgaris and other skin infections. Nadifloxacin has a
potent and broad spectrum of activity against aerobic Gram-positive and -negative bacteria
and against anaerobic bacteria. It produces significant improvement in patients with
Propionibacterium acnes infection and does not appear to cause cross-resistance to other
antibiotic agents. Its potent antimicrobial activity has also been demonstrated in the
Pseudomonas aeruginosa burn wound infection model in mice. Nadifloxacin exerts its
antibiotic activity by inhibiting the formation of supercoiled DNA by DNA gyrase. | | 化学的特性 | Off-White Crystalline Solid | | Originator | Otsuka (Japan) | | 使用 | Nadifloxacin is a topical fluorinated quinolone antibacterial used to treat skin conditions such as acne and other dermal infections caused by bacteria. This drug belongs to a class of calcium salt of polyacrylic acid crosslinked with divinyl glycol with minimal AEs. | | 定義 | ChEBI: Nadifloxacin is a pyridoquinoline, a hydroxypiperidine, a heteroarylpiperidine and a quinolone antibiotic. It has a role as an antibacterial drug. It is effective against the Gram-positive bacteria S. aureus and P. acnes, as well as Gram-negative bacteria. | | brand name | Acuatim | | 応用例（製薬） | A lipophilic tricyclic fluorobenzoquinoline with a 4- hydroxylpiperinyl moiety at the C-8 position, formulated as a cream for topical use. It is active against many Grampositive bacteria involved in skin infections, including Propionibacterium acnes (MIC 0.25–2.0 mg/L), and Staph. aureus (MIC 0.015–2 mg/L). It appears to inhibit the generation of reactive oxygen species by neutrophils. The sodium salt is used as a 1% cream for use in acne vulgaris and cutaneous staphylococcal infections. |
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