Category: piperazines

On December 31, 2011, Hu, Le-Le; Chen, Chen; Huang, Tao; Cai, Yu-Dong; Chou, Kuo-Chen published an article.COA of Formula: C17H21ClFN3O4 The title of the article was Predicting biological functions of compounds based on chemical-chemical interactions. And the article contained the following:

Given a compound, how can we effectively predict its biol. function. It is a fundamentally important problem because the information thus obtained may benefit the understanding of many basic biol. processes and provide useful clues for drug design. In this study, based on the information of chem.-chem. interactions, a novel method was developed that can be used to identify which of the following eleven metabolic pathway classes a query compound may be involved with: (1) Carbohydrate Metabolism, (2) Energy Metabolism, (3) Lipid Metabolism, (4) Nucleotide Metabolism, (5) Amino Acid Metabolism, (6) Metabolism of Other Amino Acids, (7) Glycan Biosynthesis and Metabolism, (8) Metabolism of Cofactors and Vitamins, (9) Metabolism of Terpenoids and Polyketides, (10) Biosynthesis of Other Secondary Metabolites, (11) Xenobiotics Biodegradation and Metabolism It was observed that the overall success rate obtained by the method via the 5-fold cross-validation test on a benchmark dataset consisting of 3,137 compounds was 77.97%, which is much higher than 10.45%, the corresponding success rate obtained by the random guesses. Besides, to deal with the situation that some compounds may be involved with more than one metabolic pathway class, the method presented here is featured by the capacity able to provide a series of potential metabolic pathway classes ranked according to the descending order of their likelihood for each of the query compounds concerned. Furthermore, our method was also applied to predict 5,549 compounds whose metabolic pathway classes are unknown. Interestingly, the results thus obtained are quite consistent with the deductions from the reports by other investigators. It is anticipated that, with the continuous increase of the chem.-chem. interaction data, the current method will be further enhanced in its power and accuracy, so as to become a useful complementary vehicle in annotating uncharacterized compounds for their biol. functions. A dissertation. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).COA of Formula: C17H21ClFN3O4

The Article related to carbohydrate energy lipid biol function, metabolic pathway chem interaction, Pharmacology: Methods and other aspects.COA of Formula: C17H21ClFN3O4

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

On October 1, 2020, Weatherald, Jason; Bondeelle, Louise; Chaumais, Marie-Camille; Guignabert, Christophe; Savale, Laurent; Jais, Xavier; Sitbon, Olivier; Rousselot, Philippe; Humbert, Marc; Bergeron, Anne; Montani, David published an article.Synthetic Route of 380843-75-4 The title of the article was Pulmonary complications of Bcr-Abl tyrosine kinase inhibitors. And the article contained the following:

A review. Tyrosine kinase inhibitors (TKIs) targeting the Bcr-Abl oncoprotein revolutionised the treatment of chronic myelogenous leukemia. Following the success of imatinib, second- and third-generation mols. were developed. Different profiles of kinase inhibition and off-target effects vary between TKIs, which leads to a broad spectrum of potential toxicities. Pulmonary complications are most frequently observed with dasatinib but all other Bcr-Abl TKIs have been implicated. Pleural effusions are the most frequent pulmonary complication of TKIs, usually associated with dasatinib and bosutinib. Pulmonary arterial hypertension is an uncommon but serious complication of dasatinib, which is often reversible upon discontinuation. Bosutinib and ponatinib have also been associated with pulmonary arterial hypertension, while imatinib has not. Rarely, interstitial lung disease has been associated with TKIs, predominantly with imatinib. Mechanistically, dasatinib affects maintenance of normal pulmonary endothelial integrity by generating mitochondrial oxidative stress, inducing endothelial apoptosis and impairing vascular permeability in a dose-dependent manner. The mechanisms underlying other TKI-related complications are largely unknown. Awareness and early diagnosis of the pulmonary complications of Bcr-Abl TKIs is essential given their seriousness, potential reversibility, and impact on future treatment options for the underlying chronic myelogenous leukemia. The experimental process involved the reaction of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile(cas: 380843-75-4).Synthetic Route of 380843-75-4

The Article related to review bcr abl anticancer agent myelogenous leukemia, Pharmacology: Reviews and other aspects.Synthetic Route of 380843-75-4

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

Widyastuti, Indah; Ainurofiq, Ahmad; Soewandhi, Sundani Nurono published an article in 2019, the title of the article was Effects of thermal energy, mechanical energy, and solvent on ciprofloxacin hydrochloride monohydrate physicochemical properties.SDS of cas: 86393-32-0 And the article contains the following content:

Ciprofloxacin HCl is available in the form of anhydrate and monohydrate. Water content can affect the hydrolysis, hygroscopicity, bond, and crystal properties of an active substance. This study was aimed to observe the physicochem. phenomena that occur in ciprofloxacin HCl monohydrate because of thermal energy, mech. energy, and solvent. Ciprofloxacin HCl monohydrate from two different producers were given treatments by thermal energy, mech. energy, and solvent. Afterward, the ingredients were characterized using XRD, DSC, and SEM. Other than that, crystal habit, modulus of elasticity, and dissolution were assessed. The results of characterization before and after treatment were compared to observe any changes. Ciprofloxacin HCl monohydrate from two different producers showed similarities in physicochem. properties. Manufacture treatment, which includes thermal energy, mech. energy, and solvent, affected the physicochem. characteristics of ciprofloxacin HCl monohydrate. The effect of thermal energy and solvent can change ciprofloxacin from hydrate to anhydrate, thus changed its dissolution level. Meanwhile, mech. effect by grinding and compression can decrease crystallinity and change the particle size of ciprofloxacin HCl monohydrate, thus change its dissolution level. The results of this study showed that the process of manufacturing can change the physicochem. characteristics of ciprofloxacin HCl monohydrate. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).SDS of cas: 86393-32-0

The Article related to ciprofloxacin hydrochloride monohydrate solvent thermal mech energy physicochem property, crystal structure, mechanical energy, particle size, physical and chemical properties, solvents and other aspects.SDS of cas: 86393-32-0

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

Rispal, P; Grellet, J; Celerier, C; Breilh, D; Dorian, M; Pellegrin, J L; Saux, M C; Leng, B published an article in 1996, the title of the article was Comparative uptake of sparfloxacin and ciprofloxacin into human THP 1 monocytic cells..Related Products of 86393-32-0 And the article contains the following content:

The uptake of sparfloxacin (CAS 11542-93-9) by human monocytes was studied by comparison with ciprofloxacin (CAS 86393-32-0). The human monocytic THP 1 cells were incubated with the antibiotics for 2 h. Entry of antimicrobials into the cells was determined by means of a velocity gradient centrifugation technique and HPLC assay. Antibiotic uptake was expressed as the ratio of the intracellular to the extracellular drug concentration (IC/EC). Quinolones enter readily in monocytic cells but sparfloxacin is taken up more rapidly than ciprofloxacin. At steady-state the IC/EC ratio of sparfloxacin (9.07) is higher than IC/EC of ciprofloxacin (4.29). Characterization of quinolone uptake suggests that these drugs penetrate throughout the THP 1 membrane by passive diffusion. However, the results of the present study indicate that additional mechanisms may contribute to intracellular accumulation of ciprofloxacin and sparfloxacin. Gemfibrozil, an inhibitor of organic anion transport, increases the accumulation of ciprofloxacin but does not modify IC/EC of sparfloxacin. It can be concluded that human monocyte-like cells have functional organic anion transporters and that this way of secretion is quinolone selective. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Related Products of 86393-32-0

The Article related to anti-infective agents: metabolism, cell line, chromatography, high pressure liquid, ciprofloxacin: metabolism, fluoroquinolones, gemfibrozil: pharmacology, humans, hydrogen-ion concentration, hypolipidemic agents: pharmacology, monocytes: metabolism, quinolones: metabolism and other aspects.Related Products of 86393-32-0

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

On May 14, 2015, Bruncko, Milan; Wang, Le; Sheppard, George S.; Phillips, Darren C.; Tahir, Stephen K.; Xue, John; Erickson, Scott; Fidanze, Steve; Fry, Elizabeth; Hasvold, Lisa; Jenkins, Gary J.; Jin, Sha; Judge, Russell A.; Kovar, Peter J.; Madar, David; Nimmer, Paul; Park, Chang; Petros, Andrew M.; Rosenberg, Saul H.; Smith, Morey L.; Song, Xiaohong; Sun, Chaohong; Tao, Zhi-Fu; Wang, Xilu; Xiao, Yu; Zhang, Haichao; Tse, Chris; Leverson, Joel D.; Elmore, Steven W.; Souers, Andrew J. published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity [Erratum to document cited in CA162:393666]. And the article contained the following:

On pages 2183, the authors scrambled MCL-1 helix numbering in three locations and mislabeled an amino acid in one place; the corrections are given. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to erratum structure antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On March 12, 2015, Bruncko, Milan; Wang, Le; Sheppard, George S.; Phillips, Darren C.; Tahir, Stephen K.; Xue, John; Erickson, Scott; Fidanze, Steve; Fry, Elizabeth; Hasvold, Lisa; Jenkins, Gary J.; Jin, Sha; Judge, Russell A.; Kovar, Peter J.; Madar, David; Nimmer, Paul; Park, Chang; Petros, Andrew M.; Rosenberg, Saul H.; Smith, Morey L.; Song, Xiaohong; Sun, Chaohong; Tao, Zhi-Fu; Wang, Xilu; Xiao, Yu; Zhang, Haichao; Tse, Chris; Leverson, Joel D.; Elmore, Steven W.; Souers, Andrew J. published an article.Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity. And the article contained the following:

Myeloid cell leukemia 1 (MCL-1) is a BCL-2 family protein that has been implicated in the progression and survival of multiple tumor types. Herein the authors report a series of MCL-1 inhibitors that emanated from a high throughput screening (HTS) hit and progressed via iterative cycles of structure-guided design. Advanced compounds from this series exhibited subnanomolar affinity for MCL-1 and excellent selectivity over other BCL-2 family proteins as well as multiple kinases and GPCRs. In a MCL-1 dependent human tumor cell line, administration of compound I rapidly induced caspase activation with associated loss in cell viability. The small mols. described herein thus comprise effective tools for studying MCL-1 biol. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to structure antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Application In Synthesis of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On November 30, 2021, Sarwar, M. Sohail; Ghaffar, Abdul; Huang, Qingrong published an article.Computed Properties of 86393-32-0 The title of the article was Development and characterization of sodium alginate/poly(sodium 4-styrenesulfonate) composite films for release behavior of ciprofloxacin hydrogen chloride monohydrate. And the article contained the following:

Biopolymers, in particular polysaccharides, have attracted considerable interest in the field of drug delivery due to their biodegradable and biocompatible nature. This study is focused on the preparation and characterization of drug delivery devices based on sodium alginate (SA) composite films with poly(sodium 4-styrenesulfonate) (PSS). The prepared composite films were characterized for the determination of physiochem. properties, mol. interactions, and drug release behavior. The possible intermol. hydrogen bonding between SA and PSS was determined by ATR-FTIR spectroscopy. Surface characterization was done using AFM. Polymeric films consisted of pristine SA and PSS exhibited relatively uniform and flat surfaces. However, the composite films showed phase separation that became more prominent as the concentration of PSS in the composite films was increased up to 40% (weight/weight). The contact angle (CA) values, using deionized water as a function of time (s), were ranging from 74° to 90°, and a decrease in CA (64° to 76°) was recorded for each composite film till 40 s. These CA values revealed that all the composite films were hydrophobic. It was observed that as the concentration of PSS in the films increased, hydrophobicity slightly varied as compared to the blank films of SA and PSS. Maximum CA (89°) was shown by a composite film having SA/PSS (90/10). Ciprofloxacin hydrochloride monohydrate (CPX), a model drug, loaded in a suitable composite film (crosslinked with 0.3 M CaCl2 solution) and drug release was evaluated in pH 1.2 simulated gastric fluid (SGF) and pH 7.4 phosphate buffer saline (PBS) solution In SGF, around 90% of the model drug was released in 110 min that was approx. 77% in the case of PBS. Therefore, it was concluded that a sustained drug release behavior was exhibited in SGF as compared to PBS solution These results suggest that these films are a promising and may potentially be subjected to study further their drug delivery behavior in applications like wound dressing. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Computed Properties of 86393-32-0

The Article related to sodium alginate polysodiumstyrenesulfonate composite film ciprofloxacin hydrogen chloride monohydrate, Pharmaceuticals: Drug Standards and other aspects.Computed Properties of 86393-32-0

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

Akdag, Yagmur; Sahin, Selma; Nemutlu, Emirhan; Oner, Levent published an article in 2019, the title of the article was Determination of N-acetylcysteine in the presence of ciprofloxacin or levofloxacin in microparticulate dry powder inhalers.Name: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate And the article contains the following content:

A fast and easy method was validated for simultaneous determination of ciprofloxacin hydrochloride monohydrate (CP), levofloxacin hemihydrate (LV), and N-acetylcysteine (NAC) in samples. The anal. was performed on a C18 column (250 × 4.6 mm, 5μm) (Inertsil ODS-3V) using an isocratic elution method with a mobile phase composed of 25 mM KH2 PO4 (pH 3.0) and methanol (72:28, volume/volume) at a flow rate of 1 mL/min. UV detection was performed at 214 nm for NAC and 293 nm for CP and LV. The method was validated for linearity, accuracy, precision (repeatability and reproducibility), specificity, sensitivity, and stability. The calibration study using several media demonstrated that the calibration curves were linear for all compounds in all media (R2 >0.9993). The limit of detection was 0.098μg/mL for CP, 0.049μg/mL for LV, and 0.487μg/mL for NAC. The limit of quantification was 0.328μg/mL for CP, 0.165μg/mL for LV, and 1.624μg/mL for NAC. Precision and accuracy values of the method fulfilled the required limits. All these outcomes demonstrate that the validated HPLC method is appropriate for simultaneous anal. of CP, LV, and NAC in samples for content uniformity of dry powder inhaler and permeability studies. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Name: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to lung adenocarcinoma cell dry powder inhaler ciprofloxacin levofloxacin, Pharmaceuticals: Pharmaceutics and other aspects.Name: 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

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

On January 31, 1992, Lin, Guoquan; Lu, Zhufen; Xu, Jiemei; Ouyang, Weiying published an article.Application In Synthesis of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the article was Facile salt formation of ciprofloxacin hydrochloride monohydrate. And the article contained the following:

Crude cirpofloxacin hydrochloride monohydrate was dissolved in water containing 0.09 mol concentrated HCl, decolorized with active carbon, crystallized on cooling, and recrystallized from 85% EtOH after filtration and washing with absolute EtOH; the yield was 80.7%. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Application In Synthesis of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to ciprofloxacin hydrochloride monohydrate recrystallization, Pharmaceuticals: Pharmaceutics and other aspects.Application In Synthesis of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

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

On May 1, 2006, Jiang, Xiong-Jie; Huang, Jian-Dong; Zhu, Yu-Jiao; Tang, Fen-Xiang; Ng, Dennis K. P.; Sun, Jian-Cheng published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Preparation and in vitro photodynamic activities of novel axially substituted silicon (IV) phthalocyanines and their bovine serum albumin conjugates. And the article contained the following:

Two novel axially substituted phthalocyanines, namely bis(4-(4-acetylpiperazine)phenoxy)phthalocyaninatosilicon (IV) (1) and its N-methylated derivative 2, have been synthesized. The dicationic phthalocyanine 2 is non-aggregated in water and exhibits good photophys. properties. The non-covalent BSA conjugates of these compounds have also been prepared Compound 2 and the conjugate 2-BSA show extremely high photodynamic activities toward B16 melanoma cancer cell lines. The corresponding 50% growth-inhibitory (IC50) ratios are 33 and 38 nM, resp. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to phthalocyanine albumin conjugate photodynamic therapy, Pharmaceuticals: Pharmaceutics and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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