Month: November 2022

On January 17, 2022, Lodha, Kamlesh K.; Wavhal, Deepak S.; Bhalekar, Sujit B.; Meshram, Rohan J.; Shinde, Vaishali S. published an article.Computed Properties of 67914-60-7 The title of the article was Exploring new tetrahydrothienopyridine derivatives as platelet agglutination inhibitors: synthesis, biological evaluation and In silico study. And the article contained the following:

The P2Y12 receptor is the major target for antithrombic drugs which plays a key role in platelet activation. New derivatives of 4,5,6,7-tetrahydrothieno[3,2-c]pyridine (THP) were designed targeting P2Y12 receptor. An efficient route was developed for synthesis of THP derivatives and subsequently evaluated for their antiplatelet agglutination activity. Amongst the synthesized THP derivatives (4 a-4 g), the compounds 4 a and 4 g displayed significant activity (with 88.25 and 70.17 % inhibition) as compared to other analogs and comparable with that of the reference drugs, aspirin and prasugrel. Data extracted from computational chem. techniques such as mol. docking, provided the structural rationale for the observed platelet agglutination inhibition by the newly synthesized tetrahydrothienopyridine analogs. We proposed the involvement of residues such as Cys-194 in the formation of the covalent adduct with the active metabolite of tetrahydrothienopyridine derivatives This study also put forward the possibility of the existence of an alternate pathway for metabolizing the tetrahydrothienopyridine compounds The structural data presented in this study is expected to accelerate the research on developing a tetrahydrothienopyridine scaffold as an effective antithrombotic therapeutic modality. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Computed Properties of 67914-60-7

The Article related to platelet agglutination tetrahydrothienopyridine screening antiplatelet, Placeholder for records without volume info and other aspects.Computed Properties of 67914-60-7

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

Vener, Claudia; Banzi, Rita; Ambrogi, Federico; Ferrero, Annalisa; Saglio, Giuseppe; Pravettoni, Gabriella; Sant, Milena published an article in 2020, the title of the article was First-line imatinib vs second- and third-generation TKIs for chronic-phase CML: a systematic review and meta-analysis.Product Details of 380843-75-4 And the article contains the following content:

Meta-anal. of. Imatinib, the first tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia (CML), improves overall survival (OS), but the introduction of newer TKIs requires the definition of the optimal first-line TKI for newly diagnosed Philadelphia chromosome-pos. (Ph+) chronic-phase CML. This systematic review of randomized controlled trials compares the efficacy and safety of imatinib vs second-generation (dasatinib, nilotinib, bosutinib) and third-generation TKIs (ponatinib) in adults with newly diagnosed Ph+ CP CML, concentrating on OS, progression-free survival, and hematol. and nonhematol. adverse events. The quality of the evidence was assessed using the Grading of Recommendations, Assessment, Development and Evaluation method. Two RCTs (imatinib vs nilotinib and imatinib vs dasatinib) found no difference in 5-yr OS or PFS. Second- and third-generation TKIs improved 3-mo major mol. responses (relative risk, 4.28; 95% confidence interval [RR], and other efficacy outcomes, decreased accelerated/blastic-phase transformations, but were associated with more cases of thrombocytopenia cardiovascular events and pancreatic and hepatic effects. GRADE showed that the certainty of the evidence ranged from high to moderate. This study shows that, in comparison with imatinib, second- and third-generation TKIs improve clin. responses, but the safer toxicity profile of imatinib may make it a better option for patients with comorbidities. 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 meta analysis chronic myeloid leukemia tki imatinib dasatinib ponatinib, Placeholder for records without volume info and other aspects.Product Details of 380843-75-4

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

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

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 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 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 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 June 15, 2014, Nirantar, Saurabh R.; Li, Xiang; Siau, Jia Wei; Ghadessy, Farid J. published an article.COA of Formula: C12H16N2O2 The title of the article was Rapid screening of protein-protein interaction inhibitors using the protease exclusion assay. And the article contained the following:

We have previously developed a sensitive and modular homogenous biosensor system using peptides to detect target ligands. By transposing the basic mechanistic principle of the nuclease protection assay into this biosensor framework, we have developed the protease exclusion (PE) assay which can discern antagonists of protein-protein interactions in a rapid, single-step format. We demonstrate the concept with multiple protein-peptide pairs and validate the method by successfully screening a small mol. library for compounds capable of inhibiting the therapeutically relevant p53-Mdm2 interaction. The Protease Exclusion method adds to the compendium of assays available for rapid analyte detection and is particularly suited for drug screening applications. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).COA of Formula: C12H16N2O2

The Article related to protease small mol screening biosensor p53 mdm2 protein, biosensor, high throughput screening, p53–mdm2 interaction, protein–protein interaction, Pharmacology: Structure-Activity and other aspects.COA of Formula: C12H16N2O2

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

On March 1, 2010, Sander, Kerstin; von Coburg, Yvonne; Camelin, Jean-Claude; Ligneau, Xavier; Rau, Oliver; Schubert-Zsilavecz, Manfred; Schwartz, Jean-Charles; Stark, Holger published an article.Application of 86393-32-0 The title of the article was Acidic elements in histamine H3 receptor antagonists. And the article contained the following:

Antagonists of the human histamine H3 receptor (hH3R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype. Here, we prepared compounds with acidic moieties of different pK a values to figure out that the hH3R tolerates these functionalities when added to a common pharmacophore blueprint. Depending on the acidic, electronic and steric features the designed ligands showed hH3R affinities in the nanomolar concentration range. Addnl., selected ligands were tested but failed as dual acting hH3R/hPPAR (human peroxisome proliferator-activated receptor) ligands. 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 of 86393-32-0

The Article related to h3 antagonist acidic moiety preparation structure activity crystal structure, antihistamine h3 antagonist acidic moiety preparation structure activity, Pharmacology: Structure-Activity and other aspects.Application of 86393-32-0

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