70459-17-5Relevant academic research and scientific papers
Developing ciprofloxacin analogues against plant DNA gyrase: A novel herbicide mode of action
Wallace, Michael D.,Waraich, Nidda F.,Debowski, Aleksandra W.,Corral, Maxime G.,Maxwell, Anthony,Mylne, Joshua S.,Stubbs, Keith A.
, p. 1869 - 1872 (2018/02/23)
Ciprofloxacin has been shown to exhibit potent herbicidal activity through action against plant DNA gyrase, presenting a novel mode of action. Analogues of ciprofloxacin have been prepared with increased herbicidal activity and diminished antibacterial activity, compared to ciprofloxacin, as demonstrated using model systems.
MONOCARBOXYLATE TRANSPORT MODULATORS AND USES THEREOF
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, (2016/06/20)
The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.
Synthesis of 6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid derivatives as potential antimicrobial agents
Rameshkumar, Natesh,Ashokkumar, Mohan,Subramanian, Ekambaram Harihara,Ilavarasan, Raju,Sridhar, Seshaiah Krishnan
, p. 1001 - 1004 (2007/10/03)
In the present study, a series of 1-ethyl/benzyl-6-fluoro-7-(substituted piperazin-1-yl)1,4-dihydro-4-oxo-quinoline-3-carboxylic acid were synthesized and characterized by IR, 1H-NMR, mass spectral and elemental analysis. The in vitro antibacterial and antifungal activities of the compounds were evaluated by paper disc diffusion method. The minimum inhibitory concentrations (MIC) of the compounds were also determined by agar streak dilution method. The in vivo antibacterial activity of the compounds against Escherichia coli was also evaluated by mouse protection test. All the compounds exhibited significant antibacterial and weak antifungal activities. The in vivo antibacterial activity (ED50) against E. coli was 50-160 mg kg -1 in the order of 7100 μg mL-1 against Staphylococcus aureus, Staphylococcus epidermidis, Micrococcus luteus, Bacillus cereus, E. coli, Klebsiella pneumoniae, Candida albicans and Aspergillus niger.
SOME REACTIONS OF N-PROPADIENYL-4-QUINOLONES
Radl, Stanislav,Kovarova, Lenka
, p. 2413 - 2419 (2007/10/02)
N-Alkylation of ethyl 6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (Vg) with 3-bromopropyne followed by acidic hydrolysis provided N-propynyl derivative Ic which in alkaline media yielded N-propadienyl derivative IId.Propadienyl derivatives IIa and IIb treated with primary or secondary amines provided intermediates IIIa-IIIc which were hydrolyzed to N-acetonyl derivatives IVa and IVb, respectively.N-Benzylation of ethyl 7-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylate (Va) followed by hydrolysis yielded 1-benzyl-7-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (Vd) which upon a treatment with N-methylpiperazine provided Ve.Compound Ve was hydrogenated on Pd to 6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid (Vf).
Fluoronaphthyridines and Quinolones as Antibacterial Agents. 1. Synthesis and Structure-Activity Relationships of New 1-Substituted Derivatives
Bouzard, D.,Cesare, P. Di,Essiz, M.,Jacquet, J. P.,Remuzon, P.,et al.
, p. 537 - 542 (2007/10/02)
A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated.These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position.As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin (1) or ciprofloxacin (10).Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.
Structure-Activity Relationships of Antibacterial 6,7- and 7,8-Disubstituted 1-Alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic Acids
Koga, Hiroshi,Itoh, Akira,Murayama, Satoshi,Suzue, Seigo,Irikura, Tsutomu
, p. 1358 - 1363 (2007/10/02)
Previous quantitative and qualitative structure-activity studies in antibacterial monosubstituted 1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids prompted us to synthesize the 6,7,8-polysubstituted compounds.In this paper, the preparation and antibacterial activity of the 6,7- and 7,8-disubstituted compounds and their derivatives are described.Among these compounds, 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)quinoline-3-carboxylic acid (34) possessed many significant activities and was more active than oxolinic acid (84) against Gram-positive andGram-negative bacteria.Structure activity relationships are discussed.
