Month: November 2022

Chu, Daniel T. W. published the artcileAn alternative synthesis of temafloxacin, a potent antibacterial agent, Related Products of piperazines, the main research area is temafloxacin; methylpiperazinylfluorodifluorophenyldihydrooxoquinolinecarboxylic acid; quinolinecarboxylic acid methylpiperazinylfluorodifluorophenyldihydrooxo; piperazinylphenylquinolinecarboxylic acid.

An alternative synthesis of (methylpiperazinyl)fluoro(difluorophenyl)dihydrooxoquinolinecarboxylic acid (temafloxacin) hydrochloride I, a potent antibacterial agent, was developed. The method was characterized by regiospecific displacement of the 4-fluoro of the 2,4,5-trifluoroacetophenone by 2-methylpiperazine to produce the key intermediate, 2,5-difluoro-4-(3-methylpiperazin-1-yl)acetophenone (II), which was subsequently converted to I via an intramol. nucleophilic displacement cyclization reaction.

Canadian Journal of Chemistry published new progress about temafloxacin; methylpiperazinylfluorodifluorophenyldihydrooxoquinolinecarboxylic acid; quinolinecarboxylic acid methylpiperazinylfluorodifluorophenyldihydrooxo; piperazinylphenylquinolinecarboxylic acid. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Related Products of piperazines.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Reggio, S. published the artcileCorrelation between disc potency and zone size in temafloxacin activity in vitro, Related Products of piperazines, the main research area is temafloxacin antibacterial activity determination.

A multi-test disk potency evaluation of a new fluoroquinolone, temafloxacin, has been prepared in order to evaluate the variation of the zone dimension with the disk antibiotic concentration A direct correlation between these parameters has been demonstrated. All pathogens have been isolated in hospitalized patients.

Drugs under Experimental and Clinical Research published new progress about temafloxacin antibacterial activity determination. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Related Products of piperazines.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Nakanishi, Noriyuki published the artcileIn vitro activity of temafloxacin hydrochloride (TA-167 or A-62254), a new fluorinated 4-quinolone, Related Products of piperazines, the main research area is temafloxacin antibacterial activity.

The in vitro antibacterial activity of temafloxacin HCl was evaluated against a wide variety of clin. isolates and compared with those of other fluoroquinolones. The potency (MIC90) of the compound against gram-pos. aerobic bacteria was higher or comparable to those of ciprofloxacin, ofloxacin, and norfloxacin. Against most gram-neg. enteric bacteria and Pseudomonas species, temafloxacin was less active than ciprofloxacin, but was generally as active as ofloxacin and norfloxacin, except against Proteus species and Morganella morganii. Against obligate anaerobes, it was more active than the reference quinolones. Temafloxacin was bactericidal for 1 strain each of Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. The compound inhibited E. coli DNA gyrase activity at a low concentration

Chemotherapy (Basel, Switzerland) published new progress about temafloxacin antibacterial activity. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Related Products of piperazines.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hardy, Dwight J. published the artcileComparative antibacterial activities of temafloxacin hydrochloride (A-62254) and two reference fluoroquinolones, Synthetic Route of 105784-61-0, the main research area is temafloxacin antibacterial.

The in vitro and in vivo properties of a new 1-difluorophenyl-6-fluoroquinolone, temafloxacin-HCl (I), were compared with those of difloxacin and ciprofloxacin. I was as active as ciprofloxacin and difloxacin against staphylococci and as active as ciprofloxacin and more active than difloxacin against streptococci. Against gram-neg. enteric bacteria and Pseudomonas aeruginosa, I was more active than difloxacin but less active than ciprofloxacin. The min. inhibitory concentrations of I and difloxacin were higher in urine at pH 6.5 than in broth, and those of all 3 compounds were higher in serum than in broth. When administered orally in mouse protection tests, I was as active as difloxacin and ciprofloxacin against infections with Staphylococcus aureus and streptococci. Against infections with gram-neg. enteric bacteria and P. aeruginosa, I was as active as difloxacin and ciprofloxacin. I was 3 times less active than difloxacin but was 5 times more active than ciprofloxacin against infections with Salmonella typhimurium. 2 Was as active as difloxacin and ciprofloxacin against P. aeruginosa and Proteus mirabilis pyelonephritis in mice. The peak serum concentration and serum half-life of I in mice were approx. 50% and 16%, resp., those of difloxacin after oral administration. The peak serum concentration of I in mice after oral administration was 6 times higher than that of ciprofloxacin, and the serum half-life was equal to that of ciprofloxacin.

Antimicrobial Agents and Chemotherapy published new progress about temafloxacin antibacterial. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Synthetic Route of 105784-61-0.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Barry, Arthur L. published the artcileIn vitro activities of temafloxacin, tosufloxacin (A-61827) and five other fluoroquinolone agents, Application of Temafloxacin hydrochloride, the main research area is fluoroquinolone temafloxacin tosufloxacin bacteria inhibition; A61827 fluoroquinolone comparison bacteria inhibition.

Tosufloxacin (A-61827) is the tosylate salt of A-60969 (T-3262). Temafloxacin (A-62254) is the HCl salt of A-63004. Both compounds were tested against 945 aerobic bacterial isolates and their in vitro activities were compared to those of 5 other fluoroquinolones. Ciprofloxacin and tosufloxacin were similar in their activity against the Enterobacteriaceae and Pseudomonas species. Temafloxacin and ofloxacin were similar in their activity against the Gram-neg. bacilli. Strains that were susceptible to ciprofloxacin were also susceptible to ofloxacin, temafloxacin, and tosufloxacin. Against nalidixic acid-resistant enteric bacilli, the potency of all 7 fluoroquinolones was compromised. Enoxacin and fleroxacin were the least active drugs against Gram-pos. species. Tosufloxacin was particularly active against the gram-pos. species; ciprofloxacin, difloxacin, and temafloxacin were less active.

Journal of Antimicrobial Chemotherapy published new progress about fluoroquinolone temafloxacin tosufloxacin bacteria inhibition; A61827 fluoroquinolone comparison bacteria inhibition. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Application of Temafloxacin hydrochloride.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Locatelli, Marcello published the artcileHigh performance liquid chromatography determination of prulifloxacin and five related impurities in pharmaceutical formulations, Synthetic Route of 113028-17-4, the main research area is prulifloxacin impurity determination HPLC tablet.

A novel HPLC method for the simultaneous determination of Prulifloxacin, Ulifloxacin, its process impurities in a tablets formulation and Enrofloxacin, used as Internal Standard, is developed. The separation was successfully carried out with a new stationary phase, HILIC, under isocratic elution mode using ammonium acetate buffer (5 mM, pH 5.8) and acetonitrile (12:88, volume/volume) at a flow rate of 1.0 mL/min. Column was thermostated at 25 °C (±1 °C) and 20 μL were injected for the anal. Calibration curves were linear in the investigated range with correlation coefficient better than 0.9880, while the limit of quantifications ranged from 0.25 to 5 μg/mL, depending from the analyte. The within and between batch precision (RSD%) values ranged from 0.11% to 13.9% while within and between batch trueness (bias%) values ranged from 14.0% to -11.3%. This method for the direct determination and quantification of process impurities in pharmaceutical formulations is suitable for routine analyses in quality control laboratories and was applied to evaluate for the 1st time, the presence and the quantities of cited analytes in com. available formulation.

Journal of Pharmaceutical and Biomedical Analysis published new progress about HPLC. 113028-17-4 belongs to class piperazines, name is Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate, and the molecular formula is C18H20FN3O3S, Synthetic Route of 113028-17-4.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Gu, Chong-Hui published the artcilePredicting effect of food on extent of drug absorption based on physicochemical properties, Formula: C21H19ClF3N3O3, the main research area is food drug interaction absorption surface area polarity solubility pharmacokinetics.

To develop a statistical model for predicting effect of food on the extent of absorption (area under the curve of time-plasma concentration profile, AUC) of drugs based on physicochem. properties. Logistic regression was applied to establish the relationship between the effect of food (pos., neg. or no effect) on AUC of 92 entries and physicochem. parameters, including clin. doses used in the food effect study, solubility (pH 7), dose number (dose/solubility at pH 7), calculated Log D (pH 7), polar surface area, total surface area, percent polar surface area, number of hydrogen bond donor, number of hydrogen bond acceptors, and maximum absorbable dose (MAD). For compounds with MAD ≥ clin. dose, the food effect can be predicted from the dose number category and Log D category, while for compounds with MAD < clin. dose, the food effect can be predicted from the dose number category alone. With cross validation, 74 out of 92 entries (80%) were predicted into the correct category. The correct predictions were 97%, 79%, and 68% for compounds with pos., neg. and no food effect, resp. A logistic regression model based on dose, solubility, and permeability of compounds is developed to predict the food effect on AUC. Statistically, solubilization effect of food primarily accounted for the pos. food effect on absorption while interference of food with absorption caused neg. effect on absorption of compounds that are highly hydrophilic and probably with narrow window of absorption. Pharmaceutical Research published new progress about Acidity. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Formula: C21H19ClF3N3O3.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Rolston, K. V. I. published the artcileComparative in vitro activity of the new difluoro-quinolone temafloxacin (A-62254) against bacterial isolates from cancer patients, Related Products of piperazines, the main research area is temafloxacin sensitivity bacteria cancer patient.

The in vitro activity of temafloxacin, a new difluoro quinoline agent, against 725 bacterial isolates representing 32 species was evaluated in comparison with that of ciprofloxacin. Temafloxacin inhibited the majority of Enterobacteriaceae isolates at a concentration of ≤0.5 μg/mL. It was also extremely active against Acinetobacter spp. and Aeromonas hydrophila. Its activity was 2-8 fold less than that of ciprofloxacin against most gram-neg. isolates. Methicillin-susceptible and methicillin-resistant Staphylococcus aureus, coagulase-neg. Staphylococcus spp., Streptococcus spp., Listeria monocytogenes, Bacillus spp. and group JK corynebacteria were inhibited at concentrations equal to that of ciprofloxacin.

European Journal of Clinical Microbiology & Infectious Diseases published new progress about Bacteria. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Related Products of piperazines.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Segawa, Jun published the artcileStudies on pyridonecarboxylic acids. IV. Synthesis and antibacterial activity evaluation of S-(-)- and R-(+)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids, Product Details of C18H20FN3O3S, the main research area is thiazetoquinolinecarboxylic acid synthesis antibacterial activity.

Optically active isomers of 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (NM394) were prepared through optical resolution of a racemic intermediate by high-performance liquid chromatog. The absolute configuration at the C-1 position in the thiazetoquinolone ring of the (-)-isomer was confirmed by X-ray anal. of to be S. The in vitro antibacterial activity of the (-)-isomer was 2-8 times that of the (+)-isomer.

Chemical & Pharmaceutical Bulletin published new progress about Crystal structure. 113028-17-4 belongs to class piperazines, name is Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate, and the molecular formula is C18H20FN3O3S, Product Details of C18H20FN3O3S.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hupertz, Vera published the artcileSusceptibility of Campylobacter pylori isolated from pediatric and adult patients to seven new quinolone antibiotics and nalidixic acid, Safety of Temafloxacin hydrochloride, the main research area is Campylobacter sensitivity quinolone bactericide nalidixate.

The susceptibility of 26 strains of C. pylori to 7 new quinolone antibiotics and nalidixic acid was determined All strains were resistant to nalidixic acid. Difloxacin, A-56620, A-62254, and ciprofloxacin were equally effective against the test strains with MICs ranging from 0.06 to 2.0 μg/mL. Fleroxacin, amifloxacin, perfloxacin, and norfloxacin showed only moderate activity against C. pylori. The new quinolone agents, which are bactericidal, may prove useful in the eradication of C. pylori from the gastric mucosa.

Chemotherapy (Basel, Switzerland) published new progress about Helicobacter pylori. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Safety of Temafloxacin hydrochloride.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics