著者

石綺 孝義 鈴江 清吾 入倉 勉

出版者

公益社団法人 日本化学会

雑誌

日本化学会誌(化学と工業化学) (ISSN:03694577)

巻号頁・発行日

vol.1985, no.10, pp.2054-2056, 1985-10-10 (Released:2011-05-30)

参考文献数

11

被引用文献数

3

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Reaction of 2, 3, 4, 5-tetrafluoro-1-nitrobenzene [4] with N-(ethoxycarbonyl)piperazine in aqueous ethanol gave 4-(4-ethoxycarbonyl-1-piperazinyl)-2, 3, 5-trifluoro-1-nitrobenzene [5] in 89% yield, which could be quantitatively converted into its 2-cyclopropylamino derivative [6]. Malonate [7] prepared from [6] and diethyl ethoxymethylenemalonate in 73% yield, was cyclized in the reaction with acetic anhydride and conc. sulfuric acid, accompanying elimination of the nitro group, to give [8] in 41% yield. Saponification of [8] gave quinolonecarboxylic acid [3] which possesses potent antibacterial activity both in vivo and in vitro, in 92% yield.

著者

平井 敬二 青山 博 庭田 寧 安江 徳太郎 福田 秀行 鈴江 清吾 入倉 勉

出版者

公益社団法人 日本化学療法学会

雑誌

CHEMOTHERAPY (ISSN:00093165)

巻号頁・発行日

vol.38, no.Supplement2, pp.1-10, 1990-11-30 (Released:2011-08-04)

参考文献数

7

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新キノロン系抗菌剤であるfleroxacinのin vitro抗菌力について検討した. FleroxacinはEnterobacterimeae, Neisseria spp.及びHaemophilus influenzaeに対し強い抗菌力を示し, また, staphylococci, Pseudomonas aeruginosa及びBranhamella catarrhalisに対しても良好な抗菌活性が認められた. 臨床分離株に対するfleroxacinの抗菌力はnornoxacin及びofloxacinと同程度であったが, ciprofloxacinよりは幾分劣っていた. なお, fleroxacinはmethicillin耐性Staphylococcus aureus及びgentamicin耐性P.aeruginosaに対しても優れた抗菌活性を示した. Fieroxacinの抗菌力は, 培地の種類, 培地のpH, 接種菌量, 金属イオンの添加及びヒト血清の添加による影響をほとんど受けなかった. MICとMBCはほぼ一致していた. Fleroxacinは他のキノロン剤同様Escherichia coli及びP. aeruginosaから分離したDNA gyraseのスーパーコイリング活性を強く阻害した. Fleroxacinは大腸菌, 緑膿菌, ブドウ球菌に対し良好なpost antibiotic effect (PAE) を有していた.

著者

湯浅 龍三 今井 淳 森川 裕司 草嶋 久生 内田 広 入倉 勉

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.102, no.5, pp.469-476, 1982-05-25 (Released:2008-05-30)

参考文献数

9

被引用文献数

2 6

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The presence of three kinds of hydrates of AM-715 (1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid) was confirmed by elemental analysis, Karl-Fischer method, thermogravimetric analysis, differential scanning calorimetry, infrared spectroscopy, and X-ray diffractometry. Anhydrous AM-715 was not hygroscopic under less than 36% of relative humidity, but easily transformed to 5/2-hydrate over 62-78% of relative humidity and 5-hydrate above 94% of relative humidity, at 40°C. Anhydrous AM-715 was transformed to 5/2-hydrate with the first-order kinetics and 5/2-hydrate was dehydrated according to the first-order kinetics with an activation energy of dehydration of 22 kcal/mol. The 5/2-hydrate was converted to 5-hydrate much slowly than anhydrous AM-715. Dissolution rates were determined in water by using tape procedure, showing a slight difference between anhydrous AM-715 and its hydrates. In order to determine the effect of hydration on bioavailability, the serum levels in dogs were measured after oral administration. There were no significant differences among bioavailability of anhydrous AM-715, its 5/2-hydrate and 5-hydrate.