Category: piperazines

On March 31, 1996, Rispal, Patric; Grellet, Jean; Celerier, Christophe; Breilh, Dominique; Dorian, Martine; Pellegrin, Jean Luc; Saux, Marie Claude; Leng, Bernard published an article.Safety 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 Comparative uptake of sparfloxacin and ciprofloxacin into human THP 1 monocytic cells: evidence for an organic anion transport. And the article contained the following:

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 addnl. mechanisms may contribute to intracellular accumulation of ciprofloxacin and sparfloxacin 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).Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to sparfloxacin ciprofloxacin monocyte organic anion transport, Pharmacology: Drug Metabolism and other aspects.Safety 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 February 28, 2021, Li, Huan-Ting; Zhu, Xiaoyong published an article.Electric Literature of 380843-75-4 The title of the article was Quinoline-based Compounds with Potential Activity against Drug-resistant Cancers. And the article contained the following:

A review. Drug resistance is the major cause of the failure of cancer chemotherapy, so one of the most important features in developing effective cancer therapeutic strategies is to overcome drug resistance. Quinoline moiety has become one of the most privileged structural motifs in anticancer agent discovery since its derivatives possess potent activity against various cancers including drug-resistant cancers. Several quinoline-based compounds which are represented by Anlotinib, Bosutinib, Lenvatinib, and Neratinib have already been applied in clin. practice to fight against cancers, so quinoline-based compounds are potential anticancer agents. The present short review article provides an overview of the recent advances of quinoline-based compounds with potential activity against drug-resistant cancers. The structure-activity relationship and mechanisms of action are also discussed. 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).Electric Literature of 380843-75-4

The Article related to review quinoline potential activity against drug resistant cancer, anticancer, cancers, drug resistance, mechanisms of action, quinoline, structure-activity relationship, Pharmacology: Reviews and other aspects.Electric Literature of 380843-75-4

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

Yuzbasioglu, Mebrure Burcak; Eskazan, Ahmet Emre published an article in 2021, the title of the article was Bosutinib – related pleural effusion in patients with chronic myeloid leukemia.HPLC of Formula: 380843-75-4 And the article contains the following content:

A review. Tyrosine kinase inhibitors (TKIs) are the mainstay of the current management of chronic myeloid leukemia (CML). Dasatinib is a 2GTKI, which is utilized in CML treatment both in the upfront and salvage settings Lymphocytosis pleural effusion. Bosutinib is another potent 2GTKI, which can also be used in the first- and subsequent-lines in patients with CML [20]. It is a dual Src/Abl TKI, and it exhibits minimal inhibitory activity against c-KIT or PDGFR [21]. Diarrhea is the most common AE of bosutinib therapy. 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).HPLC of Formula: 380843-75-4

The Article related to review dasatinib bosutinib anticancer agent chronic myeloid leukemia, adverse event, bosutinib, chronic myeloid leukemia, pleural effusion, tyrosine kinase inhibitor, Pharmacology: Reviews and other aspects.HPLC of Formula: 380843-75-4

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

On May 31, 2020, Casavecchia, Grazia; Galderisi, Maurizio; Novo, Giuseppina; Gravina, Matteo; Santoro, Ciro; Agricola, Eustachio; Capalbo, Silvana; Zicchino, Stefano; Cameli, Matteo; De Gennaro, Luisa; Righini, Francesca Maria; Monte, Ines; Tocchetti, Carlo Gabriele; Brunetti, Natale Daniele; Cadeddu, Cristian; Mercuro, Giuseppe published an article.Quality Control of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile The title of the article was Early diagnosis, clinical management, and follow-up of cardiovascular events with ponatinib. And the article contained the following:

A review. Abstract: Chronic myeloid leukemia (CML) is a myeloproliferative disorder characterized by neoplastic transformation of pluripotent cells due to a typical cytogenetic and mol. mutation known as Philadelphia (Ph) chromosome. In 2001, the introduction of the tyrosine kinasis inhibitor (TKI) imatinib as a therapeutic strategy for CML with PH chromosome mutation represented an important step towards treatment of these patients, and nowadays, this drug represents the gold therapeutic standard in this clin. setting. A second generation of TKIs (dasatinib, nilotinib, and bosutinib) showed an effective action in all patients with mutations resistant to imatinib. Ponatinib is a third-generation TKI and is the only inhibitor with activity against T3151 mutation. The impact of ponatinib on cardiovascular events was first evaluated in the PACE trial. We therefore report and discuss most relevant evidence currently available on cardiovascular events associated with the use of ponatinib. Though many exams can be used for diagnosis and follow-up of this kind of cardiotoxicity, echocardiog. seems to have a pivotal role thanks to its feasibility, availability, and low cost. 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).Quality Control of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to review chronic myeloid leukemia cardiovascular event diagnosis ponatinib, cardio-oncology, chronic myeloid leukemia, ponatinib, review, tyrosine kinase inhibitors, Pharmacology: Reviews and other aspects.Quality Control of 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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

On August 31, 2021, Latagliata, Roberto; Attolico, Immacolata; Trawinska, Malgorzata Monika; Capodanno, Isabella; Annunziata, Mario; Elena, Chiara; Luciano, Luigiana; Crugnola, Monica; Bergamaschi, Micaela; Bonifacio, Massimiliano; Barate, Claudia; Mauro, Endri; Binotto, Gianni; Sgherza, Nicola; Aguzzi, Chiara; Monteleone, Barbara; Sora, Federica; Caocci, Giovanni; Luzi, Debora; Mariggio, Elena; Scaffidi, Luigi; Cattaneo, Daniele; Gozzini, Antonella; Di Veroli, Ambra; Abruzzese, Elisabetta; Galimberti, Sara; Iurlo, Alessandra; Specchia, Giorgina; Breccia, Massimo published an article.Category: piperazines The title of the article was Bosutinib in the real-life treatment of chronic myeloid leukemia patients aged >65 years resistant/intolerant to previous tyrosine-kinase inhibitors. And the article contained the following:

To evaluate the role of bosutinib in elderly patients aged >65 years with chronic myeloid leukemia (CML), a real-life cohort of 101 chronic-phase CML patients followed up in 23 Italian centers and treated with bosutinib in second or a subsequent line was retrospectively evaluated. Starting dose of bosutinib was 500 mg/day in 25 patients (24.8%), 400 mg/day in 7 patients (6.9%), 300 mg/day in 33 patients (32.7%), 200 mg/day in 34 patients (33.6%), and 100 mg/day in 2 patients (2.0%). Grade 3/4 hematol. toxicity occurred in 7/101 patients (6.9%) and grade 3/4 extra-hematol. toxicity in 19/101 patients (18.8%). Permanent bosutinib discontinuation due to toxicity was needed in 12 patients (11.9%). Among the 96 patients evaluable for response, 74 (77.0%) achieved a complete cytogenetic response (CCyR), while 64 of these 74 patients in CCyR (66.6% of all 96 evaluable patients) also achieved a mol. response (MR) (major MR [MR 3.0] in 21 [21.8%], deep MR [MR 4.0/4.5] in 43 [44.8%]). Our real-life data show that bosutinib is effective, with a favorable safety profile, also in elderly patients with important comorbidities and resistance and/or intolerance to previous tyrosine-kinase inhibitor treatments. As a consequence, it could play a significant role in current clin. practice for frail patients. 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).Category: piperazines

The Article related to bosutinib anticancer agent chronic myeloid leukemia, bosutinib, chronic myeloid leukemia, elderly people, real-life clinical experience, Placeholder for records without volume info and other aspects.Category: piperazines

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

On October 31, 2022, Singh, Priya; Singh, Neelu; Mishra, Nidhi; Nisha, Raquibun; Alka; Maurya, Priyanka; Pal, Ravi Raj; Singh, Samipta; Saraf, Shubhini A. published an article.Recommanded Product: 380843-75-4 The title of the article was Functionalized bosutinib liposomes for target specific delivery in management of estrogen-positive cancer. And the article contained the following:

This study was designed to create surface-functionalized bosutinib liposomes that could be used for the management of estrogen-pos. cancers. The novelty of this work was the anti-cancer activity of bosutinib-loaded liposomes (Bos-LPs) in estrogen-pos. cancer via estrogen response elements, responsible for the malignancy of cancer cells. Biotin effectively delivers active moiety to tumor tissues because it interacts with the biotin receptor and operates through the Sodium-dependent multivitamin transporters (SMVT) transporter. The prepared liposomes had a 257.73 ± 4.50 nm particle size, – 28.07 ± 5.81 mV zeta potential, 87.78 ± 1.16 % encapsulation efficiency and 85.56 ± 0.95 % drug release for 48 h. The surface architecture of biotin-modified bosutinib-loaded liposomes (b-Bos-LPs) was confirmed using scanning electron and transmission electron microscopies. In-vitro experiments revealed that b-Bos-LPs outperformed Bos and Bos-LPs in terms of significantly reduced cell viability in MCF-7 cells. According to biodistribution and pharmacokinetic studies, b-Bos-LPs have a higher Bos concentration in tumor tissues as compared to the other organs and also possess better pharmacokinetic activity, indicating that they can be used to treat carcinogen-induced estrogen-pos. cancers. This is the first study to show that b-Bos-LPs can display activity against estrogen-pos. cancer via biotin targeting. As evidenced by various parameters, b-Bos-LPs showed improved anticancer targeting, therapeutic safety and efficacy in carcinogen-induced estrogen-pos. cancer. The receptor protein estrogen, which is primarily responsible for this cancer was downregulated by b-Bos-LPs in an immunoblotting assay. The results showed that biotinylated distearoylphosphatidylcholine (DSPC) augmented LPs loaded with Bosutinib can cause apoptosis in estrogen-pos. breast cancer and be an effective way to treat estrogen-pos. cancer. 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).Recommanded Product: 380843-75-4

The Article related to bosutinib liposome target specific delivery estrogen breast cancer, bosutinib, breast cancer, estrogen-positive, liposomes, Placeholder for records without volume info and other aspects.Recommanded Product: 380843-75-4

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

On March 5, 2021, Hu, Feng; Morris, Patrick J.; Bonaventura, Jordi; Fan, Hong; Mathews, William B.; Holt, Daniel P.; Lam, Sherry; Boehm, Matthew; Dannals, Robert F.; Pomper, Martin G.; Michaelides, Michael; Horti, Andrew G. published an article.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was 18F-labeled radiotracers for in vivo imaging of DREADD with positron emission tomography. And the article contained the following:

Designer Receptors Exclusively Activated by Designer Drugs (DREADD) are a preclin. chemogenetic approach with clin. potential for various disorders. In vivo visualization of DREADDs has been achieved with positron emission tomog. (PET) using 11C radiotracers. The objective of this study was to develop DREADD radiotracers labeled with 18F for a longer isotope half-life. A series of non-radioactive fluorinated analogs of clozapine with a wide range of in vitro binding affinities for the hM3Dq and hM4Di DREADD receptors has been synthesized for PET. Compound [18F]7b was radiolabeled via a modified 18F-deoxyfluorination protocol with a com. ruthenium reagent. [18F]7b demonstrated encouraging PET imaging properties in a DREADD hM3Dq transgenic mouse model, whereas the radiotracer uptake in the wild type mouse brain was low. [18F]7b is a promising long-lived alternative to the DREADD radiotracers [11C]clozapine ([11C]CLZ) and [11C]deschloroclozapine ([11C]DCZ). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to fluorine 18 labeled radiotracer pet imaging dreadd receptor, (18)f, chemogenetics, dreadd, pet, sar, hm3dq, hm4di, Placeholder for records without volume info and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On December 31, 2021, Saxena, Kapil; Jabbour, Elias; Issa, Ghayas; Sasaki, Koji; Ravandi, Farhad; Maiti, Abhishek; Daver, Naval; Kadia, Tapan; DiNardo, Courtney D.; Konopleva, Marina; Cortes, Jorge E.; Yilmaz, Musa; Chien, Kelly; Pierce, Sherry; Kantarjian, Hagop; Short, Nicholas J. published an article.Recommanded Product: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile The title of the article was Impact of frontline treatment approach on outcomes of myeloid blast phase CML. And the article contained the following:

The natural course of untreated chronic myeloid leukemia (CML) is progression to an aggressive blast phase. Even in the current era of BCR-ABL1 tyrosine kinase inhibitors (TKIs), the outcomes of blast phase CML remain poor with no consensus frontline treatment approach. We retrospectively analyzed the response rates and survival outcomes of 104 consecutive patients with myeloid blast phase CML (CML-MBP) treated from 2000 to 2019 based on 4 different frontline treatment approaches: intensive chemotherapy (IC) + TKI (n = 20), hypomethylating agent (HMA) + TKI (n = 20), TKI alone (n = 56), or IC alone (n = 8). We also evaluated the impact of TKI selection and subsequent allogeneic stem cell transplant (ASCT) on patient outcomes. Response rates were similar between patients treated with IC + TKI and HMA + TKI. Compared to treatment with TKI alone, treatment with IC/HMA + TKI resulted in a higher rate of complete remission (CR) or CR with incomplete count recovery (CRi) (57.5% vs 33.9%, p < 0.05), a higher complete cytogenetic response rate (45% vs 10.7%, p < 0.001), and more patients proceeding to ASCT (32.5% vs 10.7%, p < 0.01). With a median follow-up of 6.7 years, long-term outcomes were similar between the IC + TKI and HMA + TKI groups. Combination therapy with IC/HMA + TKI was superior to therapy with TKI alone, including when anal. was limited to those treated with a 2nd/3rd-generation TKI. When using a 2nd/3rd-generation TKI, IC/HMA + TKI led to lower 5-yr cumulative incidence of relapse (CIR; 44% vs 86%, p < 0.05) and superior 5-yr event-free survival (EFS; 28% vs 0%, p < 0.05) and overall survival (OS; 34% vs 8%, p = 0.23) compared to TKI alone. Among patients who received IC/HMA + TKI, EFS and OS was superior for patients who received a 2nd/3rd generation TKI compared to those who received imatinib-based therapy. In a landmark anal., 5-yr OS was higher for patients who proceeded to ASCT (58% vs 22%, p = 0.12). Compared to patients treated with TKI alone for CML-MBP, treatment with IC + TKI or HMA + TKI led to improved response rates, CIR, EFS, and OS, particularly for patients who received a 2nd/3rd-generation TKI. Combination therapy with IC + TKI or HMA + TKI, rather than a TKI alone, should be considered the optimal treatment strategy for patients with CML-MBP. 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).Recommanded Product: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

The Article related to myeloid blast phase cml frontline treatment approach, blast phase, cml, chemotherapy, hypomethylating agent, tki, Placeholder for records without volume info and other aspects.Recommanded Product: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile

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

On October 31, 2021, Huang, Hui; Zheng, Suyue; Chen, Min; Xie, Liyuan; Li, Ziyi; Guo, Min; Wang, Jianhong; Lu, Mingwei; Zhu, Xingen published an article.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide The title of the article was The potential of the P2X7 receptor as a therapeutic target in a sub-chronic PCP-induced rodent model of schizophrenia. And the article contained the following:

We studied the role of the P2X7 receptor on cognitive dysfunction in a mouse model of schizophrenia. An adult mouse model was established by treatment with phencyclidine (PCP), an N-methyl-D-aspartate (NMDA) receptor antagonist. Young mice were divided into three groups: (1) the control (saline-injected) group; (2) exptl. 5 mg/kg PCP-injected group; and (3) exptl. 10 mg/kg PCP-injected group. The mice were subjected to the open-field and Morris water maze tests at 7 wk. After i.p. injection of the P2X7 receptor antagonist JNJ-47965567, the behavior tests were performed again. Samples were taken after testing. The P2X7 receptor protein and mRNA expression levels were detected by immunohistochem., Western blotting and PCR. This study revealed that the infant sub-chronic PCP mice model showed severe spatial learning and memory impairment in the Morris water maze and schizophrenia-like symptoms (hypermotor behavior) in the open-field test. The P2X7 receptor protein was highly expressed in the sub-chronic PCP mouse model and more highly expressed in the hippocampus than the prefrontal lobe. After the P2X7 receptor was blocked with JNJ-47965567, P2X7 receptor protein and mRNA expression in the frontal lobe were significantly increased, and the spatial memory impairment and hypermotor behavior induced by PCP were reversed. PCP-induced cognitive impairment can be significantly improved by antagonizing the P2X7 receptor. Therefore, we believe that the P2X7 receptor plays an important role in the cognition of schizophrenic-like mice. The experimental process involved the reaction of N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide(cas: 1428327-31-4).Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

The Article related to schizophrenia p2x7 receptor phencyclidine jnj47965567, cognitive disorder, p2x7 receptor, pcp, schizophrenia, Placeholder for records without volume info and other aspects.Recommanded Product: N-((4-(4-Phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide

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

Beiginejad, Hadi; Rafiee, Zeinab published an article in , the title of the article was Dependence of mechanisms to thermodynamics in the electrochemical study of different electrophiles in the presence of some sulfur nucleophiles.SDS of cas: 67914-60-7 And the article contains the following content:

Abstract: Electrochem. study of different electrophiles in the presence of p-toluenesulfinic acid and 2-mercaptobenzothiazole as sulfur nucleophiles was investigated. Mechanistic study of the electrochem. reactions indicates that the electrochem. oxidation of some species in the presence of the sulfur groups has different mechanisms, but some other species in the presence of both sulfur nucleophiles have the same mechanism. To explain the reason for this difference, the computational study was used. Thermodn. investigation shows that when ΔGtot of the electrochem. oxidation of products are less than that of initial species, the electrochem. produced species can be oxidized during controlled-potential coulometry. The results of this work indicate that the computational study can be used to justify the reaction mechanisms. Cyclic voltammetry, linear sweep voltammetry, and controlled-potential coulometry were used to obtain the exptl. results. Also, by the use of BP86 level of theory and 6-31 + G(d,p) basis set, the theor. data were obtained. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).SDS of cas: 67914-60-7

The Article related to electrophile isulfur nucleophile electrochem oxidation reaction mechanism, Placeholder for records without volume info and other aspects.SDS of cas: 67914-60-7

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