Heterocyclic Building Blocks-piperazine

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 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

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 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 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 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 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

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

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

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