プルリフロキサシン

プルリフロキサシン 化学構造式
123447-62-1
CAS番号.
123447-62-1
化学名:
プルリフロキサシン
别名:
プルリフロキサシン;プルリフロキサシン (JAN);rac-(1R*)-6-フルオロ-1-メチル-7-[4-[(5-メチル-2-オキソ-1,3-ジオキソール-4-イル)メチル]ピペラジン-1-イル]-4-オキソ-4H-[1,3]チアゼト[3,2-a]キノリン-3-カルボン酸;スオード
英語名:
Prulifloxacin
英語别名:
nm441;Sword;Pruvel;Quisnon;CS-1352;AF 3012;Plumfloxacin;PRULIFLOXACIN;Prulifloxacine;Prulioxacin-d8
CBNumber:
CB5474525
化学式:
C21H20FN3O6S
分子量:
461.46
MOL File:
123447-62-1.mol
MSDS File:
SDS

プルリフロキサシン 物理性質

融点 :
211-214°C
沸点 :
633.2±65.0 °C(Predicted)
比重(密度) :
1.62±0.1 g/cm3(Predicted)
貯蔵温度 :
Sealed in dry,Store in freezer, under -20°C
溶解性:
1M NaOH:25MLに可溶、無色透明(溶媒:1mg+25mL NaOH)
酸解離定数(Pka):
5.85±0.40(Predicted)
外見 :
白色から黄色の結晶性固体。
色:
オフホワイトからペールイエロー
極大吸収波長 (λmax):
276nm(H2O)(lit.)
Merck :
14,7908
CAS データベース:
123447-62-1(CAS DataBase Reference)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
RTECS 番号 XJ0600000
HSコード  2941.90.3000
絵表示(GHS) GHS hazard pictograms
注意喚起語 警告
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H302 飲み込むと有害 急性毒性、経口 4 警告 GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 呼吸器への刺激のおそれ 特定標的臓器毒性、単回暴露; 気道刺激性 3 警告 GHS hazard pictograms
注意書き
P261 粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

プルリフロキサシン 価格 もっと(9)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01LKTP7082 プルリフロキサシン
Prulifloxacin
123447-62-1 25mg ¥9800 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01LKTP7082 プルリフロキサシン
Prulifloxacin
123447-62-1 100mg ¥15800 2024-03-01 購入
東京化成工業 P2058 プルリフロキサシン >98.0%(HPLC)(T)
Prulifloxacin >98.0%(HPLC)(T)
123447-62-1 1g ¥15500 2024-03-01 購入
東京化成工業 P2058 プルリフロキサシン >98.0%(HPLC)(T)
Prulifloxacin >98.0%(HPLC)(T)
123447-62-1 5g ¥53500 2024-03-01 購入
Sigma-Aldrich Japan SML3707 ≥98% (HPLC)
Prulifloxacin ≥98% (HPLC)
123447-62-1 10MG ¥8400 2023-06-01 購入

プルリフロキサシン 化学特性,用途語,生産方法

外観

うすい黄赤色~黄色~緑色粉末~結晶

効能

抗菌薬, 核酸合成阻害薬

商品名

スオード (Meiji Seikaファルマ)

説明

Prulifloxacin was launched as the third fluoroquinone. It was introduced in Japan as an oral treatment for urinary tract infections (UTls), respiratory tract infections (RTls) and bacterial pneumoniae. It can be synthesized in 10 steps from commercially available 3,4-difluoroaniline. Key steps involve the cyclization of 6,7-difluoro-rl-hydroxy-2- thioquinoline-3carboxylic acid ethyl ester with 1 ,I-dibromomethane to give the corresponding thiazeto-[3,2a]quinoline. Aromatic nucleophilic substitution of the 7-fluoro atom with piperazine followed by hydrolysis of the ethyl ester and finally alkylation of the piperazinyl moiety with 4-(bromomethyl)-5-methyl-l ,bdioxol-Bone complete the synthesis. Prulifloxacin is a lipophilic prodrug, which is rapidly hydrolyzed to the corresponding Ndealkylated piperazine, NM 394, by paraoxonase type enzymes in blood and liver following intestinal absorption. The DNA gyrase inhibitor NM 394 accounts for all antimicrobial activity: it shows a similar or greater activity against gram-positive bacteria compared to ciprofloxacin, and a greater activity in the case of gram-negative bacteria. In clinical studies, prulifloxacin has shown good efficacy against UTls and RTls. The drug is mainly excreted in the urine and in the feces as unchanged NM 394, which has a plasma half-life of approximately 8 h. Phototoxicity in animal models is less severe than with other quinolones. Prulifloxacin is well tolerated with an adverse effect profile similar to that of other fluoroquinolones.

化学的特性

Off-White Solid

使用

Prulifloxacin is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class. Prulifloxacin is a prodrug for active metabolite, Ulifloxacin. Antibacterial.

応用例(製薬)

A lipophilic prodrug which is very rapidly metabolized by esterase into ulifloxacin, a 6-fluoro, 7-piperazinyl thiazetoquinoline.
Ulifloxacin is moderately active against Staph. aureus (MIC 0.4–0.8 mg/L) and inactive against Str. pneumoniae (MIC 2–8 mg/L) as well as against Enterococcus spp. Against Enterobacteriaceae (MIC 0.05–0.8 mg/L) and Ps. aeruginosa (MIC 0.2–0.8 mg/L) activity is similar to that of ciprofloxacin. It is active against fastidious Gram-negative bacilli, but not against anaerobes and non-fermentative Gram-negative bacilli. Activity against Acinetobacter spp. is modest.
Prulifloxacin is rapidly converted into ulifloxacin and after 3 h is no longer detected in blood. In volunteers receiving a single oral dose, peak plasma concentrations of 0.68 mg/L (300 mg dose) to 1.88 mg/L (for 400 mg dose) were attained between 0.67 and 1.25 h. The mean apparent elimination half-life was 8 h and the mean cumulative elimination rate in urine within 48 h was 31–46%. Other inactive metabolites account for 7% of the dose. Half the administered dose is eliminated in feces within 72 h as ulifloxacin and 4% as prulifloxacin. Protein binding is 45%.

プルリフロキサシン 上流と下流の製品情報

原材料

準備製品


プルリフロキサシン 生産企業

Global( 318)Suppliers
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Henan Tianfu Chemical Co.,Ltd.
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career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
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18871490254
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Xiamen AmoyChem Co., Ltd
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+8615821988213
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CONIER CHEM AND PHARMA LIMITED
+8618523575427
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18192627656
1012@dideu.com China 3320 58
Hebei Mojin Biotechnology Co., Ltd
+8613288715578
sales@hbmojin.com China 12456 58

123447-62-1(プルリフロキサシン)キーワード:


  • 123447-62-1
  • 1h,4h-(1,3)thiazeto(3,2-a)quinoline-3-carboxylicacid,6-fluoro-1-methyl-7-(4-(
  • 3-dioxol-4-yl)methyl)-1-piperazinyl)-4-oxo-(5-methyl-2-oxo-
  • nm441
  • Prulifloxacine
  • PRULIFLOXACIN(FORRESEARCHONLY)
  • (+/-)-7-{4-[(Z)-2,3-Dihydroxy-2-butenyl]-1-piperazinyl}-6-fluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid cyclic carbonate
  • 6-Fluoro-1-methyl-7-(4-(5-methyl-2-oxo-1,3-dioxelen-4-yl)methyl-1-piperazinyl)-4-oxo-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylic acid
  • PRULIFLOXACIN
  • SEA BUCKTHORN P.E 20%
  • 6-Fluoro-1-Methyl-7-[4-[(5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl]-1-piperazinyl]-4-oxo-
  • Quisnon
  • Sword
  • Prulifloxacin (Pruvel)
  • Prulifloxacin,6-Fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, NM441
  • 6-fluoro-1-Methyl-7-(4-(5-Methyl-2-oxo-1,3-dioxelen-4-yl)Methyl-1-piperazinyl)-4-oxo-4h-(1,3)thiazeto(3
  • 6-Fluoro-1-Methyl-7-(4-((5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl)piperazin-1-yl)-4-oxo-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
  • Prulioxacin-d8
  • Prulifloxacin (+/-)-7-{4-[(Z)-2,3-Dihydroxy-2-butenyl]-1-piperazinyl}-6-fluoro-1-methyl-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid cyclic carbonate
  • 6-Fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H,4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
  • (1R)-6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-1H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid
  • Prulifloxacin(NM441,AF3013)
  • CS-1352
  • Prulifloxacin, NM 441
  • Pruvel
  • PRULIFLOXACIN 99%
  • Prulifloxacin>
  • AF 3012
  • 1H,4H-[1,3]Thiazeto[3,2-a]quinoline-3-carboxylic acid, 6-fluoro-1-methyl-7-[4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]-1-piperazinyl]-4-oxo-
  • hot selling Prulifloxacin
  • Prulifloxacin USP/EP/BP
  • プルリフロキサシン
  • プルリフロキサシン (JAN)
  • rac-(1R*)-6-フルオロ-1-メチル-7-[4-[(5-メチル-2-オキソ-1,3-ジオキソール-4-イル)メチル]ピペラジン-1-イル]-4-オキソ-4H-[1,3]チアゼト[3,2-a]キノリン-3-カルボン酸
  • スオード
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