Category: piperazines

On December 21, 2012, Amani, Amene; Nematollahi, Davood published an article.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Electrochemical Synthesis Based on the Oxidation of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone in the Presence of Nucleophiles. And the article contained the following:

Electrochem. oxidation of piperazinylphenol I (R = R1 = H) with 2-benzoxazolethiol or 2-benzothiazolethiol yielded the bis(benzoxazolethiyl)phenol I (R = R1 = 2-benzoxazolylthio) and bis(benzothiazolethiyl)phenol I (R = R1 = 2-benzothiazolylthio) in 87% and 93% yields, resp. Further electrochem. oxidation of I (R = R1 = 2-benzothiazolylthio) in the presence of p-toluenesulfinic acid (TsH) gave (tosyl)(benzothiazolylthio)quinone II (Ts = 4-MeC6H4SO2); attempted direct electrochem. synthesis of II from I (R = R1 = H), 2-benzothiazolethiol, and TsH, from I (R = R1 = 2-benzothiazolylthio) and TsH in the absence of elec. potential, and from I (R = Ts; R1 = H) and 2-benzothiazolethiol were not successful. Cyclic voltammetric measurements during the reactions of I (R = H, 2-benzothiazolylthio, Ts; R1 = H, 2-benzothiazolylthio) were used to delineate the mechanisms of formation of I (R = R1 = 2-benzothiazolylthio) and II. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to benzothiazolylthio benzoxazolylthio piperazinylphenol electrochem preparation, toluenesulfonyl benzothiazolylthio benzoquinone chemoselective electrochem preparation, electrochem oxidation piperazinylphenol benzothiazolethiol benzoxazolethiol, toluenesulfinic acid electrochem oxidation substitution benzothiazolylthio piperazinylphenol and other aspects.Name: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On October 10, 2019, Crew, Andrew P.; Hornberger, Keith R.; Wang, Jing; Dong, Hanqing; Berlin, Michael; Crews, Craig M. published a patent.SDS of cas: 1211568-27-2 The title of the patent was Preparation of bifunctional compounds as modulators of proteolysis useful for treating cancer. And the patent contained the following:

The present disclosure relates to bifunctional compounds ULM-L-PTM [the ULM = a small mol. E3 ubiquitin ligase binding moiety that binds an E3 ubiquitin ligase;the PTM = a small mol. comprising a Kirsten rat sarcoma protein (KRas) targeting moiety; the L = a bond or a chem. linking moiety connecting the ULM and the PTM] or pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs or prodrugs thereof, which find utility as modulators of Kirsten rat sarcoma protein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, inhibitors of apoptosis proteins (IAP) or mouse double-minute homolog 2 ligand which binds to the resp. E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. Over 500 title compounds were prepared E.g., a multi-step synthesis of I, starting from 2,2,5-trimethyl-4-oxo-3,8,11-trioxa-5-azatridecan-13-yl 4-methylbenzenesulfonate and 2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione, was described. The present disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein (data given for representative title compounds). Diseases or disorders that result from aggregation, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).SDS of cas: 1211568-27-2

The Article related to bifunctional compound preparation kras modulator antitumor e3 ubiquitin ligase, von hippel lindau cereblon protein bifunctional compound preparation antitumor, apoptosis protein inhibitor antitumor bifunctional compound quinazolinamine preparation, mouse double minute 2 homolog mdm2 bifunctional compound preparation and other aspects.SDS of cas: 1211568-27-2

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

On February 15, 2020, Sirim, Mustafa Mert; Krishna, Vagolu Siva; Sriram, Dharmarajan; Unsal Tan, Oya published an article.Product Details of 890092-19-0 The title of the article was Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity. And the article contained the following:

The synthesis and evaluation of some benzimidazole-acrylonitrile hybrid derivatives I [R = Me, cyclohexyl, benzyl, etc.] was described for their in-vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv. Among the derivatives studied, I [R = p-tolyl] was found to be the most active compound with MIC of 0.78μg/mL against M. tuberculosis. This was a quite good activity compared with ethambutol (MIC = 1.56μg/mL). Moreover, I [R = p-tolyl] showed 2.8 log fold reduction in bacterial count of dormant forms of mycobacterium which was more potent than first line drugs isoniazid, ciprofloxacin, rifampicin and moxifloxacin. Having activities against both active and dormant forms of M. tuberculosis, I [R = p-tolyl] may be a useful candidate for the development of new drugs to treat tuberculosis. The experimental process involved the reaction of 4-(4-Acetylpiperazin-1-yl)benzaldehyde(cas: 890092-19-0).Product Details of 890092-19-0

The Article related to benzoimidazolyl phenylpiperazinyl acrylonitrile preparation antimycobacterial activity sar lipophilicity, propanenitrile benzoimidazolyl phenylpiperazinyl preparation antimycobacterial activity sar lipophilicity, acrylonitrile, antimycobacterial activity, benzimidazole, nutrient starvation test, propanenitrile and other aspects.Product Details of 890092-19-0

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

On November 14, 2003, Tanoury, Gerald J.; Hett, Robert; Wilkinson, H. Scott; Wald, Stephen A.; Senanayake, Chris H. published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Total synthesis of (2R,4S,2’S,3’R)-hydroxyitraconazole: implementations of a recycle protocol and a mild and safe phase-transfer reagent for preparation of the key chiral units. And the article contained the following:

A convergent total synthesis of enantiomerically-pure (2R,4S,2’S,3’R)-hydroxyitraconazole is described. The left dioxolane portion of the mol. was prepared in good yield by the conversion of (4S)-2,2-dimethyl-1,3-dioxolane-4-methanol to the corresponding enantiomerically and diastereomerically-pure acetonide (2R,4R)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolane-4-methanol by a recycle protocol involving diastereoselective crystallization of the tosylate salt, followed by re-equilibration of the mother liquor and crystallization The right-hand triazolone moiety was generated by alkylation of a triazolone derivative with an enantiomerically pure cyclic sulfate [(4R,5R)-4,5-dimethyl-1,2,3-dioxathiolane 2,2-dioxide] under mild and essentially non-hazardous reaction conditions (TDA-1, K2CO3, acetonitrile). 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 hydroxyitraconazole total synthesis preparation, tda cost effective hydroxyitraconazole total synthesis preparation, alkylation tda cost effective hydroxyitraconazole total synthesis preparation, cost effective hydroxyitraconazole total synthesis preparation, asym synthesis hydroxyitraconazole preparation and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

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

On June 30, 1980, Carissimi, M.; Picciola, G.; Ravenna, F.; Gentili, P.; Carenini, G. published an article.Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride The title of the article was Antidepressant activity of cyclohexylphenoxymorpholines. And the article contained the following:

2-[(Cyclohexylphenoxy)methyl]morpholines I (R = H, alkyl, aminoalkyl, piperazinopropionyl or -propyl, benzoylalkyl; R1 = 2-, 3-, or 4-cyclohexyl) were prepared by different methods and they showed antidepressant, tranquilizer, analgesic, and spasmolytic activity; I also inhibited blood platelet aggregation. The phenoxyisopropanolamine II reacted with ClCH2COCl to yield a 2-(phenoxymethyl)morpholin-5-one, the product was reduced (LiAlH4) to give a N-benzylmorpholine derivative, and hydrogenolysis of the latter gave I (R = H, R1 = 2-cyclohexyl). The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

The Article related to morpholine phenoxymethyl preparation antidepressant, phenoxymethylmorpholine preparation antidepressant analgesic, tranquilizer phenoxymethylmorpholine preparation, spasmolytic phenoxymethylmorpholine preparation, blood platelet phenoxymethylmorpholine preparation and other aspects.Reference of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride

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

Hubicka, Urszula; Zmudzki, Pawel; Talik, Przemyslaw; Zuromska-Witek, Barbara; Krzek, Jan published an article in 2013, the title of the article was Photodegradation assessment of ciprofloxacin, moxifloxacin, norfloxacin and ofloxacin in the presence of excipients from tablets by UPLC-MS/MS and DSC.COA of Formula: C17H21ClFN3O4 And the article contains the following content:

Background: Ciprofloxacin (CIP), moxifloxacin (MOX), norfloxacin (NOR) and ofloxacin (OFL), are the antibacterial synthetic drugs, belonging to the fluoroquinolones group. Fluoroquinolones are compounds susceptible to photodegradation process, which may lead to reduction of their antibacterial activity and to induce phototoxicity as a side effect. This paper describes a simple, sensitive UPLC-MS/MS method for the determination of CIP, MOX, NOR and OFL in the presence of photodegradation products. Results: Chromatog. separations were carried out using the Acquity UPLC BEH C18 column; (2.1 × 100 mm, 1.7 μm particle size). The column was maintained at 40°C and the following gradient was used: 0 min, 95% of eluent A and 5% of eluent B; 10 min, 0% of eluent A and 100% of eluent B, at a flow rate of 0.3 mL min-1. Eluent A: 0.1% (volume/volume) formic acid in water; eluent B: 0.1% (volume/volume) formic acid in acetonitrile. The method was validated and all the validation parameters were in the ranges acceptable by the guidelines for anal. method validation. The photodegradation of examined fluoroquinolones in solid phase in the presence of excipients followed kinetic of the first order reaction and depended upon the type of analyzed drugs and coexisting substances. Photodegradation process of analyzed drugs was confirmed by differential scanning calorimetry. In addition, the identification of degradation products was carried out by mass spectrometry. Conclusion: The developed UPLC-MS/MS method enables the determination of CIP, MOX, NOR and OFL in the presence of photodegradation products and identification of photodegradation products. 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 antibacterial agent excipient photodegradation uplc msms dsc, ciprofloxacin, differential scanning calorimetry, kinetic evaluation, moxifloxacin, norfloxacin, ofloxacin, photodegradation, tandem mass spectrometry, ultra performance liquid chromatography and other aspects.COA of Formula: C17H21ClFN3O4

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

On February 1, 2020, Koller, Dora; Vaitsekhovich, Viktoryia; Mba, Cecile; Steegmann, Juan L.; Zubiaur, Pablo; Abad-Santos, Francisco; Wojnicz, Aneta published an article.Computed Properties of 380843-75-4 The title of the article was Effective quantification of 11 tyrosine kinase inhibitors and caffeine in human plasma by validated LC-MS/MS method with potent phospholipids clean-up procedure. application to therapeutic drug monitoring. And the article contained the following:

Therapeutic drug monitoring (TDM) help to improve treatment efficacy and safety. Therefore, a simple and sensitive liquid chromatog.-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous monitoring of 11 tyrosine kinase inhibitors (TKIs) in human plasma. TKIs included in the assay are used in the treatment of chronic myeloid leukemia (CML: imatinib, dasatinib, nilotinib, bosutinib, ponatinib), polycythemia vera (ruxolitinib), chronic lymphocytic leukemia (ibrutinib) and rheumatoid arthritis (filgotinib, tofacitinib, baricitinib, peficitinib). Caffeine was also included in the method. Caffeine increases the acidity of the stomach and decreases its pH as well as is a competitive inhibitor of cytochrome P 450 isoenzymes. Thus, it may influence absorption and metabolism of some TKIs, by modifying their plasma levels. The analytes of interest and their stable isotope-labeled internal standards were extracted from 200μL of human plasma. Microelution-solid phase extraction (μ-SPE) was optimized for method validation and compared to simple protein precipitation (PPT). A gradient elution on a Poroshell 120 EC-C18 column at 60°C and a flow rate of 0.5 mL/min was applied for analyte separation The anal. run lasted 8 min and it was followed by a re-equilibration time of 4 min. Dynamic multiple reaction monitoring scan in the pos. ionization mode was applied to improve method sensitivity. Endogenous plasma phospholipids can strongly affect MS anal. Hence, the monitoring of endogenous phospholipids was included in the assay. Full validation of the method was achieved, including tests of precision, accuracy, trueness, linearity, extraction recovery, matrix effect, process efficiency, stability, sensitivity (with excellent LLOQs), selectivity, identity confirmation and carry-over effect. Regarding sample cleanup, more than 91% of early eluting and more than 96% of late eluting endogenous phospholipids were eliminated by μ-SPE when compared to PPT. This method enables the simultaneous plasma monitoring of 11 TKIs and caffeine and ensures high effectiveness in phospholipids elimination. The present approach is currently used in our clin. practice, being applied to TDM of dasatinib, imatinib, nilotinib and ponatinib. TKIs plasma monitoring helps to individualize dose adjustment and manage adverse effects in CML 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).Computed Properties of 380843-75-4

The Article related to tyrosine kinase inhibitor therapeutic drug monitoring hplc mass spectrometry, blood plasma analysis, caffeine, liquid chromatography-tandem mass spectrometry, phospholipids, solid phase extraction, therapeutic drug monitoring, tyrosine kinase inhibitors and other aspects.Computed Properties of 380843-75-4

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

On February 1, 2017, Xiao, Ganyuan; Li, Yan; Qiang, Xiaoming; Xu, Rui; Zheng, Yunxiaozhu; Cao, Zhongcheng; Luo, Li; Yang, Xia; Sang, Zhipei; Su, Fu; Deng, Yong published an article.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride The title of the article was Design, synthesis and biological evaluation of 4′-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease. And the article contained the following:

A series of 4′-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50 = 4.91 μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic anal. of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Aβ1-42 aggregation and Cu2+-induced Aβ1-42 aggregation by 89.5% and 79.7% at 25 μM resp., as well as acted as a selective monoamine oxidase B inhibitor (IC50 = 0.29 μM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer’s disease. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

The Article related to aminochalcone revastigmine hybrid synthesis blood brain barrier alzheimer disease, acetylcholinesterase inhibitors, alzheimer’s disease, aβ aggregation inhibitors, chalcone carbamate derivatives, monoamine oxidase b inhibitors, multifunctional agents and other aspects.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride

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

On June 30, 2020, Pushpam, Deepam; Bakhshi, Sameer published an article.Computed Properties of 380843-75-4 The title of the article was Pharmacology of tyrosine kinase inhibitors in chronic myeloid leukemia; a clinician’s perspective. And the article contained the following:

Meta-anal. of tyrosine kinase inhibitors pharmacol. in chronic myeloid leukemia patients. Upcoming concepts and related trials in the management of chronic myeloid leukemia (CML) along with future directions have been touched upon. Evidence acquisition: PubMed, Embase, Google, Cochrane library and Medline were searched to identify relevant literature for the review. Clinicaltrial.gov was searched for upcoming data and trials. Results: There are lot of gap in pharmacokinetics and pharmacodynamics of TKI. Imatinib appears to be the safest TKI. Newer TKI’s achieve better achievement of therapeutic milestones, deeper mol. response and less chances of progression of CML compared to imatinib. Newer TKI appears to be better choice for achieving TFR. When the objective is survival, imatinib is still the TKI of choice. Primary prophylaxis with antiplatelet drugs for TKI having cardiovascular and thromboembolic side effects should be considered. Conclusion: Pharmacogenetic data of TKI is still immature to guide in therapeutic decision making in clin. practice. There is need for further research in pharmacol. and pharmacogenomics of newer TKI’s. Randomized controlled trials are required to decide the optimum TKI for TFR. Safe and effective TKI for targeting T315I mutation, CML accelerated phase and blast crisis are an active area of research. 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).Computed Properties of 380843-75-4

The Article related to meta analysis chronic myeloid leukemia tyrosine kinase pharmacol, gene polymorphism and imatinib, pharmacology of tyrosine kinase inhibitors, selection of tyrosine kinase inhibitors, tyrosine kinase inhibitors in chronic myeloid leukemia and other aspects.Computed Properties of 380843-75-4

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

On June 30, 2021, Mizuno, Takahito; Sakai, Takamasa; Tanabe, Kouichi; Kozaki, Koji; Umemura, Takumi; Higashikawa, Mariko; Kimura, Tomoki; Yamada, Tetsuya; Goto, Nobuyuki; Ohtsu, Fumiko published an article.Category: piperazines The title of the article was Identification of target small molecule tyrosine kinase inhibitors that need monitoring and clinical application of protocol for early detection of cancer therapeutics-related cardiac dysfunction using signal detection: An investigation of real world data. And the article contained the following:

Purpose: In order to detect cancer therapeutics-related cardiac dysfunction (CTRCD) early, we identified which drugs were to be monitored using signal detection and the package insert, and created and applied a protocol to address this. Methods: Adverse event data recorded in the Japanese Adverse Drug Event Report (JADER) database between Apr. 2004 and Jan. 2018 were used. We applied our findings clin. by creating a protocol to detect CTRCD early. All cases at Tosei General Hospital where the target tyrosine kinase inhibitors were administered from when they were first released in Nov. 2019 were included. We compared the results from before and after we began the protocol to clarify its effects. Results: We found that CTRCD was not described in the serious side-effect section of the package inserts for Bosutinib, Alectinib, and Osimertinib even though CTRCD signals were detected for them. Therefore, it is possible that we may have previously overlooked CTRCD. When we applied our protocol using Osimertinib as the target drug, we were able to detect CTRCD early in 5/21 (24%) patients. Conclusions: It was clarified that the drug identification method used in this study for early detection of adverse events leads to early detection of adverse events when applied clin. 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 cancer cardiac dysfunction tyrosine kinase inhibitor therapeutics side effect, cancer therapeutics-related cardiac dysfunction, japanese adverse drug event report database, osimertinib, small molecule tyrosine kinase inhibitors and other aspects.Category: piperazines

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