Category: piperazines

Food and Drug Administration, HHS published the artcileList of drug products that have been withdrawn or removed from the market for reasons of safety or effectiveness, Product Details of C21H19ClF3N3O3, the main research area is drug safety effectiveness standard.

The Food and Drug Administration (FDA) is amending its regulations to include a list of drug products that may not be used for pharmacy compounding under the exemptions under section 503A of the Federal Food, Drug, and Cosmetic Act because they have had their approval withdrawn or were removed from the market because the drug product or its components have been found to be unsafe or not effective. The list has been compiled under the new statutory requirements of the Food and Drug Administration Modernization Act of 1997 (Modernization Act).

Federal Register published new progress about Adrenal cortex (extracts). 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Product Details of C21H19ClF3N3O3.

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

Wang, Ning-Yu published the artcileDesign, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors, Application In Synthesis of 109384-27-2, the main research area is thienopyrimidine piperazinone preparation SAR non Hodgkin lymphoma PI3K antiproliferative; Antiproliferative activity; PI3Kδ; Piperazinone; SAR; Thieno[3,2-d]pyrimidine.

Two classes of piperazinone-containing thieno[3,2-d]pyrimidines were designed and synthesized as new PI3Kδ inhibitors in this study. Detailed SAR study with respect to the piperazinone substituents at the 6-position of thieno[3,2-d]pyrimidine core demonstrated that piperazinone-containing thieno[3,2-d]pyrimidines would be more potent and selective for PI3Kδ than their piperazine counterparts, which led to the discovery of several potent PI3Kδ inhibitors with comparable or better antiproliferative activity against a panel of non-Hodgkin lymphoma (NHL) cell lines as compared with idelalisib. Our study will promote the development of new PI3Kδ inhibitors based on piperazinone-containing thieno[3,2-d]pyrimidine scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiproliferative agents. 109384-27-2 belongs to class piperazines, name is 1-Methylpiperazin-2-one hydrochloride, and the molecular formula is C5H11ClN2O, Application In Synthesis of 109384-27-2.

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

Ali, Ayad K. published the artcileSignal detection and clarification of peripheral neuropathy and Guillain-Barracue syndrome associated with exposure to systemic fluoroquinolones, Formula: C21H19ClF3N3O3, the main research area is Cipro Levaquin Avelox Noroxin Floxin fluoroquinolone Guillain Barre syndrome.

Aims: Peripheral neuropathy (PN) is an identified risk of systemic antibacterial therapy with fluoroquinolones. The risk and its severity, including the development of Guillain-Barré syndrome (GBS) between individual agents is uncertain. This study examines the association between fluoroquinolones and PN and GBS in cases spontaneously reported to the FDA Adverse Event Reporting System (FAERS). Study Design: Retrospective pharmacovigilance anal. Place and Duration of Study: Cases submitted to FAERS between 1997 and 2012. Methodol.: The MedDRA Preferred Term was used to define PN and GBS. Individual fluoroquinolones were identified by generic names and route of administration. Empirical Bayes Geometric Mean (EBGM) with 95% confidence interval (EB05-EB95) was calculated as disproportionality measure. Safety signals with EB05≥2 was considered a significant disproportional increase in event reporting of at least twice times higher than expected. Results: There were 539 PN reports out of 46,257 adverse event reports submitted for fluoroquinolones. 9% of PN reports were for GBS. Significant disproportionality of PN (EBGM 2.70; EB05-EB95 2.51-2.90) and GBS (EBGM 3.22; EB05-EB95 2.55-4.02) was identified for fluoroquinolones. Signals of PN were detected for ciprofloxacin (EBGM 3.24; EB05-EB95 2.87-3.66) and levofloxacin (EBGM 3.36; EB05-EB95 3.02-3.72). A GBS signal was detected for ciprofloxacin (EBGM 4.15; EB05-EB95 2.94-5.74). GBS and PN resp. ranked 6th and 8th among reported neurol. events. Conclusion: This study reemphasizes the link between fluoroquinolones and PN, and shows potential association with more severe forms of nerve damage, e.g. GBS. Unless the benefit of fluoroquinolone therapy outweighs PN risk, treatment with alternative antibacterial agents is recommended.

British Journal of Pharmaceutical Research published new progress about Antibacterial agents. 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

Ozaki, Masakuni published the artcileIn vivo antibacterial activity of a prodrug of NM394, a thiazetoquinoline carboxylic acid derivative, Recommanded Product: Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate, the main research area is thiazetoquinoline prodrug NM441 NM394 antibacterial.

NM394 (6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid) has potent, broad-spectrum antibacterial activity in vitro, but not in vivo. To increase the bioavailability of NM394, various prodrugs were synthesized and tested. One of them, NM441, an N-(5-methyl-2-oxo-1,3-dioxol-4-yl) derivative, showed potent in vivo antibacterial activity. Using thin-layer chromatog.-bioautog., it was confirmed that after oral administration, NM441 was readily absorbed and hydrolyzed to NM394. Other prodrugs of NM394 were only partially metabolized to NM394. In pharmacokinetic studies in mice and monkeys, it was found that the blood levels of NM394 were 7.8 and 5.9 × greater, resp., when NM441 rather than NM394 was administered. These findings suggest that NM441 is an effective prodrug of NM394.

Chemotherapy (Basel) published new progress about Antimicrobial agents. 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, Recommanded Product: Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate.

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

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

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

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

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

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