オゼノキサシン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 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。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P302+P352：皮膚に付着した場合：多量の水と石鹸で洗うこと。

  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。

オゼノキサシン 価格

オゼノキサシン 化学特性,用途語,生産方法

• 用途

  オゼノキサシンは、主に尋常性ざ瘡（にきび）の治療で使用されるニューキノロン（フルオロキノロン）系の抗菌剤であり、細菌性の皮膚感染症にも使用される。

• 効能

  抗菌薬, 核酸合成阻害薬

• 商品名

  ゼビアックス (マルホ)

• 説明

  Ozenoxacin is a novel, nonfluorinated quinolone antibiotic discovered by Toyama Chemical Co. Ltd. and developed by Maruho Co. Ltd. Ozenoxacin was approved by the PMDA of Japan in September 2015 for the treatment of acne and skin infections. Ozenoxacin shows potent antibacterial activity against anaerobic and aerobic, gram-positive and -negative bacteria, especially those implicated in superficial skin infections such as S. aureus, Staphylococcus epidermidis, and Propionibacterium acnes. The mechanism of action of ozenoxacin involves the drug’s affinity for DNA gyrase and DNA topoisomerase IV and upon binding triggers bacterial apoptosis.

• 使用

  Ozenoxacin is a non-fluorinated topical quinolone. It exhibits antimicrobial activity against?propionibacteria and staphylococci. Ozenoxacin can be used to treat acne and superficial skin infections.

• 合成

  A U.S. patent filed by co-workers at Toyama describes the only publicly disclosed synthetic approach to this drug.12 The drug?ˉs assembly hinges upon a key Stille coupling between a quinolonyl bromide and a stannylpyridine. Buchwald-Hartwig coupling of commercially available 2,6- dibromotoluene (22) and cyclopropylamine (23) gave Ncyclopropyl- 3-bromo-2-methylaniline 24 in 84% yield , and this step was followed by reaction with diethyl ethoxymethylenemalonate (25) and subsequent cyclization under acidic conditions to secure bromoquinoline 26 in 43% yield over the two-step sequence. Stille coupling of 27 with bromoquinoline 26 resulted in pyridyl quinoline adduct 28 in 80% yield. Saponification of ester 28 followed by acidic removal of the N-acetyl group delivered the active pharmaceutical ingredient ozenoxacin (III) in 75% yield.
  The preparation of key stannane 27, which is not commercially available and began with the conversion of commercially available 5-bromo-2- chloro-3-methylpyridine (30) to aminopyridine derivative 31 upon treatment with aqueous methylamine at elevated temperature in a sealed vessel. The resulting aminopyridine was subjected to acetic anhydride in pyridine, resulting in acetamide 32 in good yield, and this coupling was followed by a modest-yielding palladium-catalyzed installation of the stannyl group to deliver subunit 27.

  

オゼノキサシン 生産企業

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