- Synthesis and crystal structure of 1-cyclopropyl-6,7-difluoro-8-methoxy-4- oxo-1,4-dihydro-3-quinoline carboxylic acid-(O3,O4)-bis-(acetate-O)borate
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The crystal structure of the 1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1, 4-dihydro-3-quinoline carboxylic acid-(O3,O4)-bis-(acetate-O)borate has been determined by single crystal X-ray diffraction method. The crystal belongs to monoclinic with space group P2(1)/n, with a = 16.818(9), b = 6.585(4), c = 18.663(4)?, a = 90, b = 107.351(7), g = 90, V = 1972.8(18)?3, Z = 4, Dx = 1.479 Mg/m3, l(MoKa) = 0.128, F(000) = 908, ?(MoKa) = 0.128 mm-1, R = 0.1083 and wR = 0.3062 for 2378 reflections with I > 2s(I). The two rings of fluoroquinolone and borate ring are almost coplanar with dihedral angles values lower than 2. The crystal structure is stabilized by intermolecular hydrogen bonds and p-p stacking interactions.
- Li, Fei,Zhang, Jie,Jiang, Yu,Jin, Lei,Zhang, Chuan
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- COMPOUNDS TARGETING RNA-BINDING PROTEINS OR RNA-MODIFYING PROTEINS
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The invention relates to a compound represented by Formula (I): or a pharmaceutically acceptable salt thereof, compositions comprising the same and methods of preparing and using the same. The variables are described herein.
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- Compound and preparation method thereof
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The invention provides a compound and a preparation method of the compound, wherein the compound has the structure as shown in the formula 1, and the compound is taken as a standard substance or a reference substance, therefore, the quality of moxifloxacin raw medicines and preparation products can be effectively controlled.
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Paragraph 0067; 0068; 0069
(2018/03/24)
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- IR, FT-ICR-MS studies on (1′S, 6′S)-1-cyclopropyl-7-(2,8- diazabicyclo[4.3.0] non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3- carboxylic acid hydrochloride salt
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The infrared spectra of (1′S, 6′S)-1-cyclopropyl-7-(2,8- diazabicyclo[4.3.0] non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3- carboxylic acid hydrochloride salt (CLF-HCl) were studied and compared with free base. Their fragmentation pathways were investigated using tandem mass spectrometric (MS/MS) techniques on Fourier-transform ion cyclotron resonance spectrum, and many characteristic fragment ions were found.
- Lin, Zhiwei
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p. 254 - 258
(2013/12/04)
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- Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3β
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The synthesis, GSK-3β inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone- 3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this class were potent and highly selective GSK-3 inhibitors.
- Cociorva, Oana M.,Li, Bei,Nomanbhoy, Tyzoon,Li, Qiang,Nakamura, Ayako,Nakamura, Kai,Nomura, Masahiro,Okada, Kyoko,Seto, Shigeki,Yumoto, Kazuhiro,Liyanage, Marek,Zhang, Melissa C.,Aban, Arwin,Leen, Brandon,Szardenings, Anna Katrin,Rosenblum, Jonathan S.,Kozarich, John W.,Kohno, Yasushi,Shreder, Kevin R.
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scheme or table
p. 5948 - 5951
(2011/10/18)
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- Synthesis and antimycobacterial evaluation of newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids
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Thirty-four newer 1-cyclopropyl-1,4-dihydro-6-fluoro-7-(substituted secondary amino)-8-methoxy-5-(sub)-4-oxoquinoline-3-carboxylic acids were synthesized from 1,2,3,4-tetrafluoro benzene and evaluated for in vitro and in vivo antimycobacterial activities against Mycobacterium tuberculosis H37Rv (MTB), multi-drug resistant M. tuberculosis (MDR-TB) and Mycobacterium smegmatis (MC2) and also tested for the ability to inhibit the supercoiling activity of DNA gyrase. Among the synthesized compounds, 7-(1-(4-methoxybenzyl)-3,4,5,6,7,8-hexahydroisoquinolin-2(1H)-yl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-5-nitro-4-oxoquinoline-3-carboxylic acid (13n) was found to be the most active compound in vitro with MIC of 0.16 and 0.33 μM against MTB and MDR-TB, respectively. In the in vivo animal model 13n decreased the bacterial load in lung and spleen tissues with 2.54 and 2.92 - log10 protections, respectively, at the dose of 50 mg/kg body weight. Compound 13n also inhibited the supercoiling activity of mycobacterial DNA gyrase with IC50 of 30.0 μg/ml.
- Senthilkumar, Palaniappan,Dinakaran, Murugesan,Banerjee, Debjani,Devakaram, Ruth Vandana,Yogeeswari, Perumal,China, Arnab,Nagaraja, Valakunja,Sriram, Dharmarajan
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p. 2558 - 2569
(2008/09/21)
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- PROCESS FOR THE PREPARATION OF GATIFLOXACIN AND REGENERATION OF DEGRADATION PRODUCTS
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The subject of the present invention are an improved synthesis process comprising a process for regeneration of a side product of gatifloxacin and an analysis method for process control in the synthesis of gatifloxacin (Formula I).
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Page/Page column title page; 4; 12-13
(2008/06/13)
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- ANTIMICROBIAL QUINOLONES, THEIR COMPOSITIONS AND USES
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Compounds of the following formula (I) are effective antimicrobial agents.
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- Antimicrobial quinolones, their compositions and uses
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Compounds of the following formula: 1are effective antimicrobial agents.
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- 1,4-dihydro-4-oxo-3-quinoline derivatives as selectively toxic mammalian antibacterial agents
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Compounds of the formula STR1 and the pharmaceutically acceptable salts thereof, wherein Q, X and R are as defined below. The compounds of formula I are broad spectrum mammalian antibacterial agents and exhibit favorable selectivity against procaryotic cells.
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- Quinoline-3-carboxylic acid derivatives
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Compounds of formula (I): STR1 (in which R1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.
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- 8-alkoxyquinolonecarboxylic acid and salts thereof
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Quinolonecarboxylic acid derivatives of the following formula: STR1 wherein R indicates a hydrogen atom or lower alkyl group, R1 indicates a lower alkyl group, R2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, STR2 (here, n is 0 or 1, R3 indicates a hydrogen atom or lower alkyl group, R4 indicates a hydrogen atom, lower alkyl group and R5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.
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