- Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections
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Delafloxacin, a fourth-generation anionic fluoroquinolone (FQ) was approved in 2019 for community acquired bacterial pneumonia (CARP). It has broad spectrum activity and an improved class-related toxicity profile. However, it has recently failed a Phase 3
- Betson, Mark,Bingham, Matilda,Doyle, Paul,Hallworth, Sebastian,Harvey, Rebecca,Huxley, Anthony,Kirk, Ralph,Moat, John,Nelson, Gary,Pesnot, Thomas,Tait, Michael
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- Preparation method of sitafloxacin intermediate
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The invention discloses a preparation method of a sitafloxacin intermediate, wherein the preparation method includes the steps: in the presence of low-valence metals or transition metals, 3-chloro-2,4,5-trifluorobenzoyl chloride undergoes a reaction with
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Paragraph 0037; 0040; 0041; 0044
(2019/02/13)
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- Preparation method of Delafloxacin and intermediates thereof
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The invention relates to a preparation method of Delafloxacin and intermediates thereof. The method comprises the following steps: firstly, taking 3-chloro-2,4,5-fluorobenzoic acid (compound 1) as a raw material and reacting the raw material with thionyl
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Paragraph 0018; 0041-0043
(2018/08/04)
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- Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety
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A series of novel 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety were synthesized and evaluated for their biological activity. Our results reveal that compounds 9a-9c have considerable activity against both of MTB H37Rv ATCC 27294 (MICs: 3.81-7.13 μg/mL) and methicillin-sensitive Staphylococcus aureus strains (MICs: 0.008-0.5 μg/mL).
- Huang, Ju,Wang, Minghua,Wang, Bin,Wu, Zhaoyang,Liu, Mingliang,Feng, Lianshun,Zhang, Jun,Li, Xiaoning,Yang, Yang,Lu, Yu
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supporting information
p. 2262 - 2267
(2016/04/20)
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- Synthesis and bioactivity of 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives
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A series of 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives was prepared and examined for cardiotonic activity. The structures of these new pyridazinone derivatives were confirmed by IR, 1H-NMR and mass spectrum. The cardiotonic activities of these compounds were studied on isolated perfused toad heart and compared with the activity of levosimendan (CAS 141505-33-1). Compound 5a emerged as the most interesting compound in this series with potential cardiotonic activity. ECV Editio Cantor Verlag.
- Wang, Teng,Dong, Ying,Wang, Li-Chen,Chen, Zhen
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p. 641 - 646
(2008/03/11)
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- 2,3,4,5-tetrahalogenobenzene derivatives
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2,3,4,5-trihalogenobenzene derivatives of the formula STR1 in which R is --COOH, --COCl, --COF, --CN, --CONH2, --CH2 OH, --CH2 Cl, --CHCl2, --CCl3 or --CHO, R1 is H, Cl or F, and R2 is Cl or F, it only being possible for R1 or R2 to be F, and processes for their preparation starting from benzonitriles reacted with potassium fluoride. The novel compounds are intermediates for antibacterials such as quinolone carboxylic acids.
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- Process for the synthesis of 3-chloro-2,4,5-trifluorobenzoic acid
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An improved process for the preparation of 3-chloro-2,4,5-trifluorobenzoic acid is described which involves reaction of a diester of 3,4,5,6-tetrafluoro-1,2-benzenedicarboxylic acid with a substituted amine to afford 3-amino-2,4,5-trifluorobenzoic acid followed by subsequent conversion of the amio intermediate into 3-chloro-2,4,5-trifluorobenzoic acid.
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- Antibacterial agents
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Novel quinoline-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
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