Category: piperazines

On March 31, 2020, Omsland, Maria; Andresen, Vibeke; Gullaksen, Stein-Erik; Ayuda-Duran, Pilar; Popa, Mihaela; Hovland, Randi; Brendehaug, Atle; Enserink, Jorrit; McCormack, Emmet; Gjertsen, Bjorn Tore published an article.Product Details of 380843-75-4 The title of the article was Tyrosine kinase inhibitors and interferon-a increase tunneling nanotube (TNT) formation and cell adhesion in chronic myeloid leukemia (CML) cell lines. And the article contained the following:

Chronic myeloid leukemia (CML) is a stem cell disease of the bone marrow where mechanisms of inter-leukemic communication and cell-to-cell interactions are proposed to be important for optimal therapy response. Tunneling nanotubes (TNTs) are novel intercellular communication structures transporting different cargos with potential implications in therapy resistance. Here, we have investigated TNTs in CML cells and following treatment with the highly effective CML therapeutics tyrosine kinase inhibitors (TKIs) and interferon-a (IFNa). CML cells from chronic phase CML patients as well as the blast crisis phase cell lines, Kcl-22 and K562, formed few or no TNTs. Treatment with imatinib increased TNT formation in both Kcl-22 and K562 cells, while nilotinib or IFNa increased TNTs in Kcl-22 cells only where the TNT increase was associated with adherence to fibronectin-coated surfaces, altered morphol., and reduced movement involving beta1integrin. Ex vivo treated cells from chronic phase CML patients showed limited changes in TNT formation similarly to bone marrow cells from healthy individuals. Interestingly, in vivo nilotinib treatment in a Kcl-22 s.c. mouse model resulted in morphol. changes and TNT-like structures in the tumor-derived Kcl-22 cells. Our results demonstrate that CML cells express low levels of TNTs, but CML therapeutics increase TNT formation in designated cell models indicating TNT functionality in bone marrow derived malignancies and their microenvironment. 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).Product Details of 380843-75-4

The Article related to imatinib nilotinib antineoplastic agent chronic myeloid leukemia tnt ifnalpha, cell adhesion, chronic myeloid leukemia, interferon-α, tunneling nanotubes, tyrosine kinase inhibitors and other aspects.Product Details of 380843-75-4

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

On September 27, 2017, Beyzavi, Hudson; Mandal, Debashis; Strebl, Martin G.; Neumann, Constanze N.; D’Amato, Erica M.; Chen, Junting; Hooker, Jacob M.; Ritter, Tobias published an article.Formula: C12H16N2O2 The title of the article was 18F-Deoxyfluorination of Phenols via Ru π-Complexes. And the article contained the following:

The deficiency of robust and practical methods for 18F-radiofluorination is a bottleneck for positron emission tomog. (PET) tracer development. Here, we report the first transition-metal-assisted 18F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atm., large substrate scope, and translatability to generate doses appropriate for PET imaging. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to transition metal assisted deoxyfluorination phenol ruthenium complex, crystal mol structure fluorophenyl ruthenium cyclopentenyl complex, radiofluorination phenol ruthenium complex and other aspects.Formula: C12H16N2O2

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

On October 31, 1980, Carissimi, M.; Picciola, G.; Ravenna, F.; Carenini, G.; Gentili, P. published an article.Computed Properties of 59695-29-3 The title of the article was 2-(2-Thienyl)morpholines active on the central nervous system. And the article contained the following:

Morpholinones I [R = H, PhCH2, CHMe2, substituted 3-(1-piperazinyl)propionyl, substituted 3-(1-piperazinyl)propyl; Z = O] underwent LiAlH4 reduction to yield I (Z = H2), which showed antidepressant activity. Cyclocondensation of 2-benzylamin-1-(2-thienyl)ethanol with ClCH2COCl gave I (R = PhCH2, Z = 0). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Computed Properties of 59695-29-3

The Article related to morpholine thienyl preparation antidepressant, thienylmorpholine preparation antidepressant, analgesic thienylmorpholine preparation, antiinflammatory thienylmorpholine preparation and other aspects.Computed Properties of 59695-29-3

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

On November 1, 2015, Dong, Yan; Li, Kehuang; Xu, Zhixiang; Ma, Haikuo; Zheng, Jiyue; Hu, Zhilin; He, Sudan; Wu, Yiyuan; Sun, Zhijian; Luo, Lusong; Li, Jiajun; Zhang, Hongjian; Zhang, Xiaohu published an article.Category: piperazines The title of the article was Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors. And the article contained the following:

The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC50 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chem., plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Category: piperazines

The Article related to protein palmitoyltransferase porcupine antagonist synthesis inhibitor wnt signaling secretion, antagonist, cancer therapy, porcupine, scaffold hybridization, wnt signaling pathway and other aspects.Category: piperazines

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

On April 20, 2016, Ziff, Jeannie; Rudolph, Dale A.; Stenne, Brice; Koudriakova, Tatiana; Lord, Brian; Bonaventure, Pascal; Lovenberg, Timothy W.; Carruthers, Nicholas I.; Bhattacharya, Anindya; Letavic, Michael A.; Shireman, Brock T. published an article.COA of Formula: C28H32N4O2S The title of the article was Substituted 5,6-(Dihydropyrido[3,4-d]pyrimidin-7(8H)-yl)-methanones as P2X7 Antagonists. And the article contained the following:

We describe the synthesis of a novel class of brain penetrating P2X7 antagonists with high potency at both the rat and human P2X7 receptors. Disclosed herein are druglike mols. with demonstrated target engagement of the rat P2X7 receptors after an oral dose. Specifically, compound 20 occupied the P2X7 receptors >80% over the 6 h time course as measured by an ex vivo radioligand binding experiment In a dose-response assay, this mol. has a plasma EC50 of 8 ng/mL. Overall, 20 has suitable druglike properties and pharmacokinetics in rat and dog. This mol. and others disclosed herein will serve as addnl. tools to elucidate the role of the P2X7 receptor in neuropsychiatric disorders. 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).COA of Formula: C28H32N4O2S

The Article related to dihydropyrido pyrimidinyl methanone derivative preparation p2x7 antagonist, 5,6-dihydropyrido[3,4-d]pyrimidin-7(8h)-yl) methanones, cns, il-1β, p2x7, depression, neuroinflammation and other aspects.COA of Formula: C28H32N4O2S

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

On August 30, 2020, Yu, Shihui; Yuan, Huiya; Chai, Guihong; Peng, Kuan; Zou, Peizhi; Li, Xuxi; Li, Jian; Zhou, Fanfan; Chan, Hak-Kim; Zhou, Qi Tony published an article.Product Details of 86393-32-0 The title of the article was Optimization of inhalable liposomal powder formulations and evaluation of their in vitro drug delivery behavior in Calu-3 human lung epithelial cells. And the article contained the following:

Inhalation therapy has advantages for the treatment of multidrug resistant bacterial lung infections with high drug concentrations at the infection sites in the airways and reduced systemic exposure. We have developed liposomal formulations for pulmonary delivery of synergistic ciprofloxacin (Cipro) and colistin (Col) as the potential candidate for treatment of lung infections caused by multidrug resistant Gram-neg. bacteria. This study aims to: (1) further optimize the powder formulation by adding drying stabilizers (polyvinyl pyrrolidone or poloxamer) to protect the liposomes during spray-freeze-drying; (2) evaluate the transport and cellular uptake of drugs in a human lung epithelial Calu-3 cell model. The liposomal powder formulations were produced using the ultrasonic spray-freeze-drying technique. The optimal formulation (F5) used mannitol (8% w/v) and sucrose (2% w/v) as the internal lyoprotectants. Adding external lyoprotectants/aerosolization enhancers (i.e. 8% w/v mannitol, 2% w/v sucrose and 1%, weight/weight PVP 10) produced the superior rehydrated EE values of ciprofloxacin and colistin (50.2 ± 0.9% for Cipro and 37.8 ± 1.2% for Col) as well as satisfactory aerosol performance (FPF: 34.2 ± 0.8% for Cipro and 33.6 ± 0.9% for Col). The cytotoxicity study indicated that F5 with the colistin concentration at 50μg/mL and ciprofloxacin at 200μg/mL was not cytotoxic to human lung epithelial Calu-3 cells. The intracellular uptake of ciprofloxacin was concentration-dependent in Calu-3 cells and the uptake of A-B was more than that of B-A for all samples (p < 0.05). This study demonstrates that co-delivery of ciprofloxacin and colistin in a single liposome can lower the transport capability of both drugs across the Calu-3 cell monolayer and their accumulation in the cells. These findings indicate that co-loaded liposomal powder of ciprofloxacin and colistin is a promising potential treatment for respiratory infections caused by multidrug resistant Gram-neg. bacteria. 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).Product Details of 86393-32-0

The Article related to ciprofloxacin colistin sustained release liposome inhalation aerosol uptake, aerosol performance, calu-3 cell monolayer, ciprofloxacin, colistin, drug transport, liposomal powder and other aspects.Product Details of 86393-32-0

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

On March 31, 2020, Ly, Diane; Dongol, Anjila; Cuthbertson, Peter; Guy, Thomas V.; Geraghty, Nicholas J.; Sophocleous, Reece A.; Sin, Lucia; Turner, Bradley J.; Watson, Debbie; Yerbury, Justin J.; Sluyter, Ronald published an article.Application of 1428327-31-4 The title of the article was The P2X7 receptor antagonist JNJ-47965567 administered thrice weekly from disease onset does not alter progression of amyotrophic lateral sclerosis in SOD1G93A mice.. And the article contained the following:

Abstract: The ATP-gated P2X7 ion channel has emerging roles in amyotrophic lateral sclerosis (ALS) progression. Therefore, the current study aimed to determine whether the CNS-penetrant P2X7 antagonist, JNJ-47965567, could ameliorate ALS progression in SOD1G93A mice. A flow cytometric assay revealed that JNJ-47965567 impaired ATP-induced cation dye uptake in a concentration-dependent manner in murine J774 macrophages. Female and male SOD1G93A mice were injected i.p. with JNJ-47965567 (30 mg/kg) or 2-(hydroxypropyl)-beta-cyclodextrin (vehicle control) three times a week from disease onset until end stage, when tissues were collected and studied. JNJ-47965567 did not impact weight loss, clin. score, motor (rotarod) coordination or survival compared to control mice. NanoString anal. revealed altered spinal cord gene expression in JNJ-47965567 mice compared to control mice, but such differences were not confirmed by quant. PCR. Flow cytometric analyses revealed no differences between treatments in the frequencies or activation status of T cell or dendritic cell subsets in lymphoid tissues or in the concentrations of serum cytokines. Notably, serum IL-27, IFNbetaand IL-10 were present in relatively high concentrations compared to other cytokines in both groups. In conclusion, JNJ-47965567 administered thrice weekly from disease onset did not alter disease progression or mol. and cellular parameters in SOD1G93A 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).Application of 1428327-31-4

The Article related to amyotrophic lateral sclerosis p2x7 receptor antagonist jnj47965567, amyotrophic lateral sclerosis, motor neurone disease, nqo1, p2x7 receptor, purinergic receptor, sod1g93a mice and other aspects.Application of 1428327-31-4

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

Peng, Xiaoyuan; Ma, Yiyang; Wang, Qiyang; Gao, Yanchun; Li, Guangyi; Jiang, Chenyi; Gao, Yun; Feng, Yong published an article in 2021, the title of the article was Serum amyloid a correlates with the osteonecrosis of femoral head by affecting bone metabolism.Recommanded Product: 4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile And the article contains the following content:

Osteonecrosis of femoral head (ONFH) is a progressive hip joint disease without disease-modifying treatment. Lacking understanding of the pathophysiol. process of ONFH has become the humper to develop therapeutic approach. Serum amyloid A (SAA) is an acute phase lipophilic protein during inflammation and we found that SAA is increased for the first time in the serum of ONFH patients through proteomic studies and quant. verified by ELISA. Treating rBMSCs with SAA inhibited the osteogenic differentiation via Wnt/β-catenin signaling pathway deactivation and enhanced the adipogenic differentiation via MAPK/PPARγ signaling pathway activation. Finally, bilateral critical-sized calvarial-defect rat model which received SAA treated rBMSCs demonstrated reduction of bone formation when compared to untreated rBMSCs implantation control. Hence, SAA is a vital protein in the physiol. process of ONFH and can act as a potential therapeutic target to treat ONFH. 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 proteome serum amyloid osteonecrosis femoral head bone, mapk/pparγ signaling pathway, osteonecrosis of femoral head, proteomics, serum amyloid a, wnt/β-catenin signaling pathway 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

Davis, Terry C.; Arnold, Connie L.; Mills, Glenn; Lesser, Glenn J.; Brown, W. Mark; Schulz, Richard; Weaver, Kathryn E.; Pawloski, Pamala A. published an article in 2021, the title of the article was Assessment of Oral Chemotherapy Nonadherence in Chronic Myeloid Leukemia Patients Using Brief Measures in Community Cancer Clinics: A Pilot Study.Related Products of 380843-75-4 And the article contains the following content:

The purpose of this pilot study was to assess Chronic Myeloid Leukemia (CML) patients adherence to, beliefs about, and barriers to oral anticancer agents (OAC) using brief self-report measures in community-based cancer clinics. Patients completed a structured interview including a health literacy assessment, a Brief Medication Questionnaire, two single-item self-report adherence questions, and the Medications Adherence Reasons Scale. Of the 86 participants, 88.4% were white; 55.8% male; mean age, 58.7 years; and 22.1% had limited health literacy. Nonadherence (missing at least one dose in the last week) was reported by 18.6% of participants and associated (p < 0.003) with less-than-excellent perceived ability to take CML medications (16.3%). Black participants reported more difficulty taking CML medications than white participants (28.6% vs. 8.3%, p = 0.053). Among all participants, 43.0% reported their CML medicine was ineffective and 24.4% that taking CML pills was somewhat to very hard. The most common reasons for missing a dose were simply missed it (24.4%) and side effects (18.6%). Most patients perceived their ability to take CML medication was good to excellent, yet nearly one in five reported missing at least one dose in the last week. Brief, no-cost self-report assessments to screen CML patients OAC adherence, barriers, and beliefs could facilitate counseling in busy community cancer clinics. 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).Related Products of 380843-75-4

The Article related to imatinib nilotinib dasatinib anticancer agent chronic myeloid leukemia, antineoplastic agents, chronic myelogenous leukemia, health literacy, medication adherence, self-report and other aspects.Related Products of 380843-75-4

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

On June 30, 2004, Liu, Chaomei; Xu, Fan; Liang, Shuang; Sun, Qingyan; Jiang, Yuanying published an article.HPLC of Formula: 67914-60-7 The title of the article was Synthesis and antifungal activities of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted group-2-propanols. And the article contained the following:

The title compounds 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols, e.g. I, and 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted sulfur ether-2-propanols, e.g. II, were synthesized through the reaction of an intermediate epoxide and 4-alkyloxyphenylpiperazines or substituted sulfur alcs. The structures were confirmed by the elementary anal., 1H-MR and IR spectra. MIC80 of all the title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using the RPMI1640 test medium. The results of the preliminary antifungal test show that all the title compounds exhibited potent antifungal activities to a certain extent. The antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols was more potent than that of 1-(1H,1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted sulfur ether-2-propanols in vitro. The antifungal activities of the four compounds in 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(4-alkyloxyphenylpiperazin-1-yl)-2-propanols are more potent than that of fluconazole or equal to that of ketoconazole in vitro. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).HPLC of Formula: 67914-60-7

The Article related to alkyloxyphenylpiperazinyl sulfur ether substituted triazolyl difluorophenyl propanol preparation, triazolyl difluorophenyl propanol antifungal activity fungal infection msbar and other aspects.HPLC of Formula: 67914-60-7

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