94695-52-0Relevant academic research and scientific papers
Carbostyril carboxylic compounds and intermediates, preparation method and application thereof
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, (2017/07/12)
The invention discloses carbostyril carboxylic compounds and hydrochlorides thereof and also discloses a preparation method of the compounds and the hydrochlorides thereof as well as an application of the compounds and the hydrochlorides thereof in preparing gram-positive bacterium-preventing or gram-negative bacterium-preventing drugs. Moreover, the invention discloses intermediates for preparing the compounds and a preparation method of the intermediates.
Process for the preparation of fluoroquinolonecarboxylic acids
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, (2008/06/13)
Fluoroquinolonecarboxylic acids can be prepared by hydrolysis of the corresponding C1-C4-alkyl esters with addition of water, acetic acid, and sulfuric acid using a drastically reduced amount of sulfuric acid if, relative to 1 mol of C1-C4-alkyl fluoroquinolonecarboxylate, less than 30 g of sulfuric acid are employed, the reaction mixture is heated to reflux for 0.5 to 8 hours, then a mixture of acetic acid, C1-C4-alkyl acetate, C1-C4-alkyl alcohol, and optionally water is distilled off, and finally the fluoroquinolonecarboxylic acid prepared is isolated.
4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivative as antibacterial agents
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, (2008/06/13)
Novel naphthyridine-, quinoline- and benzoxazinecarboxylic 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.
1-Substituted 7--1-pyrrolidinyl>-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic Acids. New Quantitative Structure-Activity Relationships at N1 for the Quinolone Antibacterials
Domagala, John M.,Heifetz, Carl L.,Hutt, Marland P.,Mich, Thomas F.,Nichols, Jeffry B.,et al.
, p. 991 - 1001 (2007/10/02)
A series of 18 1-substituted 7--1-pyrrolidinyl>-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (N1 analogues of CI-934) was synthesized and evaluated for antibacterial activity and DNA-gyrase inhibition.Correlations between the inhibition of DNA gyrase and antibacterial potency were established.A quantitative structure-activity relationship (QSAR) was derived by using the antibacterial potency of each of 11 strains of bacteria and the Gram-negative mean.The equations indicated that antibacterial potency was strongly dependent on STERIMOL length and width and the level of unsaturation of the N1 substituent.Some strains also showed a dependence on the presence of heteroatoms (O, N, S) in the N1 group.No significant correlations between gyrase inhibition and correlations of these parameters were found.These QSAR results are discussed in conjunction with the conformational analyses from molecular modeling studies.The substituent that most enhanced the activity of the quinolone in all regards was the cyclopropyl group.This analogue, 1-cyclopropyl-7--1-pyrrolidinyl>-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid (PD 117558), demonstrated outstanding broad spectrum activity both in vitro and in vivo when compared to relevant standards.
Antibacterial agents
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, (2008/06/13)
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.
Process for tetrafluorobenzoic acid
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, (2008/06/13)
An improved process for the preparation of 2,3,4,5-tetrafluorobenzoic acid is described which involves decarboxylation of tetrafluorophthalic acid in the presence of a base catalyst. Also described is an improved method for preparing tetrafluorophthalic acid and, in turn, a one-pot process for tetrafluorobenzoic acid using the combination of the two improvements.
Cycloaracylation of Enamines, I. - Synthesis of 4-Quinolone-3-carboxylic Acids
Grohe, Klaus,Heitzer, Helmut
, p. 29 - 37 (2007/10/02)
Starting with o-halobenzoyl chlorides 4 and open-chain secondary enamines 5, a new synthesis of 4-quinolone-3-carboxylic acids 12 is described.The reaction of 7-haloquinolone-3-carboxylic acids 12a-k with aliphatic amines 14 produces highly active antibacterial 7-aminoquinolone-3-carboxylic acids 15.The main product of the 1-cyclopropyl series, "ciprofloxacin" (15a), is being developed as a broad-spectrum chemotherapeutic agent.
Antibacterial agents
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, (2008/06/13)
Novel naphthyridine-, quinoline- and benzoxazine-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.
1-cyclopropyl-6,7-dihalo-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid and their esters, useful as intermediates for preparing the 7-amine substituted naphthyridines
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, (2008/06/13)
1-cyclopropyl-6,7-dihalo-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acids and their esters, which are useful as intermediates for the preparation of compounds which are useful as anti-bacterial agents.
