Relevant bibliographies by topics / Piperazine Synthesis

Contents

  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic 'Piperazine Synthesis'

Author: Grafiati
Published: 11 December 2022
Last updated: 25 January 2023

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles

Select a source type:

Consult the lists of relevant articles, books, theses, conference reports, and other scholarly sources on the topic 'Piperazine Synthesis.'

Next to every source in the list of references, there is an 'Add to bibliography' button. Press on it, and we will generate automatically the bibliographic reference to the chosen work in the citation style you need: APA, MLA, Harvard, Chicago, Vancouver, etc.

You can also download the full text of the academic publication as pdf and read online its abstract whenever available in the metadata.

Journal articles on the topic "Piperazine Synthesis"

1

Kmoníček, Vojtěch, Martin Valchář, and Zdeněk Polívka. "Some 4-Substituted 1-(3-Pyridylmethyl)piperazines with Antihistamine Activity." Collection of Czechoslovak Chemical Communications 59, no. 10 (1994): 2343–50. http://dx.doi.org/10.1135/cccc19942343.

Full text
Abstract:
Several compounds derived from nicotinic acid were prepared within a more extensive programme aiming at the synthesis of new substances with expected antihistamine and antidepressant activity. Some of these compounds display certain structural resemblance with the antidepressant agent piberaline (EGYT 475, Trelibet®, I) and its analogues. The products were used as intermediates for the synthesis of further compounds and most of them were subjected to pharmacological testing. Substituted nicotinic acid piperazides IIa - IId and IVa - IVe were obtained by reactions of nicotinoyl chloride (prepared in situ) with the correspondingly substituted piperazines. Reduction of the piperazides IIa - IId and IVa - IVd with diborane in situ in tetrahydrofuran afforded corresponding 1-substituted 4-(3-pyridylmethyl)piperazines IIIa - IIId and Va - Vd. Whereas the alkylation of 1-(2-pyrimidinyl)piperazine with 2-(chloromethyl)pyridine in ethanol in the presence of triethylamine resulted in compounds Ve, compound Vf was obtained by the addition reaction of 1-(3-pyridylmethyl)piperazine to acrylamide. The piperazides VIe and VIf were prepared by reactions of 2-(3-pyridyl)acetic acid with 1-(2-pyrimidinyl)piperazine or 3-(1-piperazinyl)propionamide in N,N-dimethylformamide in the presence 1,1'-carbonyldiimidazole. A similar procedure starting from nicotinic acid afforded the piperazide IVf. Compounds Vc and Vd showed significant affinity for the histamine H1-receptors (inhibition of binding of 2 nmol/l [3H]mepyramine in membranes from the rat brain: Vc, IC50 = 28 nmol/l; Vd, IC50 = 148 nmol/l). They also proved active in test of histamine aerosol in guinea pigs (PD50 = 4.1 mg/kg p.o. for compound Vc and 2.4 for compound Vd). Results of a more detailed pharmacological testing of these compounds will be published elsewhere.
APA, Harvard, Vancouver, ISO, and other styles
2

Gettys, Kristen, Zhishi Ye, and Mingji Dai. "Recent Advances in Piperazine Synthesis." Synthesis 49, no. 12 (April 25, 2017): 2589–604. http://dx.doi.org/10.1055/s-0036-1589491.

Full text
Abstract:
Piperazine ranks as the third most common N-heterocycle appearing in small-molecule pharmaceuticals. This review highlights recent advances in methods development for the construction of the piperazine­ ring system with particular emphasis on preparing carbon-substituted piperazines.1 Introduction2 Reduction of (Di)ketopiperazine3 N-Alkylation4 Transition-Metal-Catalyzed/Mediated Piperazine Synthesis4.1 The SnAP and SLAP Methods4.2 Palladium-Catalyzed Cyclization4.3 Gold-Catalyzed Cyclization4.4 Other Metal-Catalyzed/Mediated Cyclization4.5 Borrowing Hydrogen Strategy4.6 Imine Reductive Cyclization5 Reduction of Pyrazines6 Miscellaneous7 Conclusion
APA, Harvard, Vancouver, ISO, and other styles
3

Hafeez, Freeha, Ameer Fawad Zahoor, Azhar Rasul, Asim Mansha, Razia Noreen, Zohaib Raza, Kulsoom Ghulam Ali, Ali Irfan, and Gamal A. El-Hiti. "Ultrasound-Assisted Synthesis and In Silico Modeling of Methanesulfonyl-Piperazine-Based Dithiocarbamates as Potential Anticancer, Thrombolytic, and Hemolytic Structural Motifs." Molecules 27, no. 15 (July 26, 2022): 4776. http://dx.doi.org/10.3390/molecules27154776.

Full text
Abstract:
Piperazine-based dithiocarbamates serve as important scaffolds for numerous pharmacologically active drugs. The current study investigates the design and synthesis of a series of dithiocarbamates with a piperazine unit as well as their biological activities. Under ultrasound conditions, the corresponding piperazine-1-carbodithioates 5a–5j were synthesized from monosubstituted piperazine 2 and N-phenylacetamides 4a–4j in the presence of sodium acetate and carbon disulfide in methanol. The structures of the newly synthesized piperazines were confirmed, and their anti-lung carcinoma effects were evaluated. A cytotoxic assay was performed to assess the hemolytic and thrombolytic potential of the synthesized piperazines 5a–5j. The types of substituents on the aryl ring were found to affect the anticancer activity of piperazines 5a–5j. Piperazines containing 2-chlorophenyl (5b; cell viability = 25.11 ± 2.49) and 2,4-dimethylphenyl (5i; cell viability = 25.31 ± 3.62) moieties demonstrated the most potent antiproliferative activity. On the other hand, piperazines containing 3,4-dichlorophenyl (5d; 0.1%) and 3,4-dimethylphenyl (5j; 0.1%) rings demonstrated the least cytotoxicity. The piperazine with the 2,5-dimethoxyphenyl moiety (5h; 60.2%) showed the best thrombolytic effect. To determine the mode of binding, in silico modeling of the most potent piperazine (i.e., 5b) was performed, and the results were in accordance with those of antiproliferation. It exhibits a similar binding affinity to PQ10 and an efficient conformational alignment with the lipophilic site of PDE10A conserved for PQ10A.
APA, Harvard, Vancouver, ISO, and other styles
4

Durand, Carolina, and Michal Szostak. "Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization." Organics 2, no. 4 (October 8, 2021): 337–47. http://dx.doi.org/10.3390/org2040018.

Full text
Abstract:
Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diversity of piperazines is limited, with about 80% of piperazine-containing drugs containing substituents only at the nitrogen positions. Recently, major advances have been made in the C–H functionalization of the carbon atoms of the piperazine ring. Herein, we present an overview of the recent synthetic methods to afford functionalized piperazines with a focus on C–H functionalization.
APA, Harvard, Vancouver, ISO, and other styles
5

Yadav, Pradeep, and Y. C. Joshi. "Synthesis and Spectral Study of Novel Norfloxacin Derivatives." E-Journal of Chemistry 5, s2 (2008): 1154–58. http://dx.doi.org/10.1155/2008/357073.

Full text
Abstract:
Reaction of [1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinolone-3-carboxylic acid (norfloxacin) with thiazole / benzothiazole diazonium chloride to get new piperazine substituted norfloxacin derivative. These norfloxacin derivatives were further condensed with variousβ-diketone to get novel acid derivatives of 1-Ethyl-6-fluoro-4-oxo-7- [4 (thiazol-2-yldiazenyl)-piperzin-1-yl]-1,4-dihydro-quinoline-3-carboxylic acid (6a-e) and 7-(4-(benzo[d]thiazol-2-yldiazenyl)piperazin-1-yl)-1-ethyl-6-fluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (6 f-j). Structures of these compounds were established on the basis of spectral studies viz. IR,1H NMRetc.
APA, Harvard, Vancouver, ISO, and other styles
6

O’Malley, Karen, and Keith Vaughan. "Synthesis and Characterization of a Series of 1-Aryl-4-[Aryldiazenyl]-piperazines. Part II1. 1-Aryl-4-(2-Aryl-1-Diazenyl)-piperazines with Fluoro-, chloro-, Methyl-, Cyano- and Acetyl Substituents in The 1-Aryl Group." Open Chemistry Journal 3, no. 1 (May 31, 2016): 42–55. http://dx.doi.org/10.2174/1874842201603010042.

Full text
Abstract:
This paper reports the synthesis and characterization of eight series of 1-aryl-4-(2-aryl-1-diazenyl)-piperazines (12 to 19). Several series of these triazenes have been synthesized by the diazotization of a primary arylamine followed by diazonium coupling with a secondary arylpiperazine . The arylpiperazines used in this study are: 1-phenylpiperazine, 1-(4-fluorophenyl-)piperazine, 1-(4-chlorophenyl-)piperazine, 1-(3,4-dichlorophenyl-)piperazine, 1-(2-methylphenyl-)-piperazine, 1-(4-acetophenyl-)-piperazine, 1-(2-pyridyl-)piperazine and 2-cyanophenylpiperazine. These new triazenes (series 12-19) have been identified with a cocktail of contemporary spectroscopic techniques, notably infra-red and nuclear magnetic spectroscopy, supported by high resolution electron ionization mass spectrometry.
APA, Harvard, Vancouver, ISO, and other styles
7

Little, Vanessa Renee, and Keith Vaughan. "Synthesis and characterization of several series of 4-acyl-1-[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 92, no. 9 (September 2014): 838–48. http://dx.doi.org/10.1139/cjc-2014-0242.

Full text
Abstract:
Five series of a novel class of 4-acyl-1-[2-aryl-1-diazenyl]piperazines have been synthesized and characterized: the 4-acetyl-1-[2-aryl-1-diazenyl]piperazines [series 1]; the 4-cyclohexylcarbonyl-1-[2-aryl-1-diazenyl]piperazines [series 2]; the 4-benzoyl-1-[2-aryl-1-diazenyl]piperazines [series 3]; the benzyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 4]; and the t-butyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 5]. The compounds were synthesized by diazotization of a primary aromatic amine and subsequent coupling to an appropriate secondary amine: 1-acetylpiperazine [series 1]; 1-(cyclohexylcarbonyl)-piperaizine [series 2]; 1-benzoylpiperazine [series 3]; benzyl 1-piperazinecarboxylate [series 4]; and t-butyl piperazine-1-carboxylate (1-BOC-piperazine) [series 5]. The compounds of series 1–5 were characterized by 1H NMR, 13C NMR, high-resolution MS and IR spectroscopy. The model compounds 1,4-di[2-aryl-1-diazenyl]piperazines, and ethyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates were used to facilitate the assignment of the chemical shifts specific to the piperazine ring carbons. HSQC spectra of select compounds established the correlation between proton and carbon resonance signals.
APA, Harvard, Vancouver, ISO, and other styles
8

Penjisevic, Jelena, Vladimir Sukalovic, Deana Andric, Goran Roglic, Irena Novakovic, Vukic Soskic, and Sladjana Kostic-Rajacic. "Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines." Journal of the Serbian Chemical Society 81, no. 4 (2016): 347–56. http://dx.doi.org/10.2298/jsc151021097p.

Full text
Abstract:
A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates 1-(2-methoxyphenyl)-4-(piperidin-4-yl)piperazine and 1-(2-methoxyphenyl)-4-(piperidin-4-ylmethyl)piperazine. Biological evaluation of the synthesized compounds was pointed out for seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl)piperidin-4-yl]methyl}piperazine had the highest affinity for the dopamine D2 receptor. For all seven selected compounds docking analysis was performed in order to establish their structure-to-activity relationship.
APA, Harvard, Vancouver, ISO, and other styles
9

Kafka, Stanislav, Jan Čermák, Tomáš Novák, František Pudil, Ivan Víden, and Miloslav Ferles. "Syntheses of piperazines substituted on the nitrogen atoms with allyl, propyl, 2-hydroxypropyl and 3-hydroxypropyl groups." Collection of Czechoslovak Chemical Communications 50, no. 5 (1985): 1201–11. http://dx.doi.org/10.1135/cccc19851201.

Full text
Abstract:
The paper describes synthesis of 1,4-diallylpiperazine (I), 1-allylpiperazine (III), 1-propylpiperazine (IV), 1-(1-piperazinyl)-2-propanol (V), 3-(1-piperazinyl)-1-propanol (VI), 1-allyl-4-propylpiperazine (VII), 1-(4-allyl-1-piperazinyl)-2-propanol (VIII), 3-(4-allyl-1-piperazinyl)-1-propanol (IX), 1,4-dipropylpiperazine (X), 1-(4-propyl-1-piperazinyl)-2-propanol (XI), 3-(4-propyl-1-piperazinyl)-1-propanol (XII), 1,4-bis(2-hydroxypropyl)piperazine (XIII), 3-[4-(2-hydroxypropyl)-1-piperazinyl]-1-propanol (XIV) and 1,4-bis(3-hydroxypropyl)piperazine (XV). Retention indices of I-XV reported and mass spectra of the compounds are discussed.
APA, Harvard, Vancouver, ISO, and other styles
10

Magriotis, Plato A. "Recent progress toward the asymmetric synthesis of carbon-substituted piperazine pharmacophores and oxidative related heterocycles." RSC Medicinal Chemistry 11, no. 7 (2020): 745–59. http://dx.doi.org/10.1039/d0md00053a.

Full text
Abstract:
The piperazine drugs are mostly N-substituted compared to only a few C-substituted drugs. To explore this unknown chemical space, asymmetric syntheses of C-substituted piperazines is the subject of this review.
APA, Harvard, Vancouver, ISO, and other styles
More sources

Dissertations / Theses on the topic "Piperazine Synthesis"

1

Kuleya, Chipo. "The synthesis, analysis and characterisation of piperazine based drugs." Thesis, Anglia Ruskin University, 2014. https://arro.anglia.ac.uk/id/eprint/579889/1/Thesis%20%20final%20-%20Chipo%20Kuleya%20July%202015.pdf.

Full text
Abstract:
This study developed a GC-MS method for the simultaneous detection of piperazines and congeners in street samples of amphetamine type stimulants. This research investigated the clandestine routes of synthesis and chemical profiles of phenylpiperazines, represented by 1- (4-fluorophenyl)piperazine (4-FPP) and 1-(3-trifluoromethylphenyl)piperazine (3-TFMPP). These drugs are part of the increasingly prevalent illicit new psychoactive substances. The presence of (2, 3, 4) FPP and (2, 3, 4) TFMPP positional isomers has been identified by other researchers as a limitation due to their similar chemical profiles. The method was optimized and confirmed as compliant with the International Conference on Harmonisation and the Center for Drug Evaluation and Research guidelines on validation. 4- FPP and 3-TFMPP were synthesised using potential routes for clandestine laboratories. Simple extraction and analysis of 11 street samples was conducted using the method developed. Furthermore, the stability of 22 drugs during analysis was investigated. Limits of detection were in the range 5 – 1.95ng/mL free base on column. The synthesised samples were identified as 4-FPP and 3-TFMPP. Several impurities were observed in the synthesised samples, which were identified and categorised as residual reactants, isomers of 4-FPP and of 3-TFMPP and by-products of synthesis. The percentage yields of the synthesised samples obtained were up to 82.4% 4-FPP and 78.7% 3-TFMPP. The street samples were found to contain MDMA, 3-TFMPP, BZP, caffeine, ephedrine and other impurities. The analytical method simultaneously separates 19 of the most common drugs found in piperazine samples and achieves for the first time the GC-MS separation of (i) 2-FPP, 3-FPP and 4-FPP and (ii) 2-TFMPP, 3-TFMPP and 4-TFMPP at the same time from a sample matrix containing all the 19 compounds. This method provides operational laboratories with a more effective method for the chemical characterisation of street samples of piperazines and also provides novel stability data.
APA, Harvard, Vancouver, ISO, and other styles
2

Kuleya, Chipo. "The synthesis, analysis and characterisation of piperazine based drugs." Thesis, Anglia Ruskin University, 2014. http://arro.anglia.ac.uk/579889/.

Full text
Abstract:
This study developed a GC-MS method for the simultaneous detection of piperazines and congeners in street samples of amphetamine type stimulants. This research investigated the clandestine routes of synthesis and chemical profiles of phenylpiperazines, represented by 1- (4-fluorophenyl)piperazine (4-FPP) and 1-(3-trifluoromethylphenyl)piperazine (3-TFMPP). These drugs are part of the increasingly prevalent illicit new psychoactive substances. The presence of (2, 3, 4) FPP and (2, 3, 4) TFMPP positional isomers has been identified by other researchers as a limitation due to their similar chemical profiles. The method was optimized and confirmed as compliant with the International Conference on Harmonisation and the Center for Drug Evaluation and Research guidelines on validation. 4- FPP and 3-TFMPP were synthesised using potential routes for clandestine laboratories. Simple extraction and analysis of 11 street samples was conducted using the method developed. Furthermore, the stability of 22 drugs during analysis was investigated. Limits of detection were in the range 5 – 1.95ng/mL free base on column. The synthesised samples were identified as 4-FPP and 3-TFMPP. Several impurities were observed in the synthesised samples, which were identified and categorised as residual reactants, isomers of 4-FPP and of 3-TFMPP and by-products of synthesis. The percentage yields of the synthesised samples obtained were up to 82.4% 4-FPP and 78.7% 3-TFMPP. The street samples were found to contain MDMA, 3-TFMPP, BZP, caffeine, ephedrine and other impurities. The analytical method simultaneously separates 19 of the most common drugs found in piperazine samples and achieves for the first time the GC-MS separation of (i) 2-FPP, 3-FPP and 4-FPP and (ii) 2-TFMPP, 3-TFMPP and 4-TFMPP at the same time from a sample matrix containing all the 19 compounds. This method provides operational laboratories with a more effective method for the chemical characterisation of street samples of piperazines and also provides novel stability data.
APA, Harvard, Vancouver, ISO, and other styles
3

Gao, Rong. "DESIGN, SYNTHESIS AND EVALUATION OF NOVEL MUSCARINIC LIGANDS." Diss., Temple University Libraries, 2013. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/232219.

Full text
Abstract:
Pharmaceutical Sciences
Ph.D.
Muscarinic receptors are G-protein-coupled receptors that mediate the response to acetylcholine released from parasympathetic nerves. Although five mAChR subtypes (M1-M5) share a high degree of homology, they display different physiological effects including controlling smooth muscle tone to neurotransmitter release in the CNS. Hence these receptor subtypes have been investigated as potential therapeutic targets for agents capable of treating Alzheimer's Disease, Parkinson's Disease, peptic ulcer disease, COPD, urinary incontinence, and muscle spasms. Our interest in the development of subtype selective muscarinic ligands led to previous reports detailing the identification of substituted lactones as lead muscarinic compounds. Later work involved molecular modifications of those leads that included the addition of aromatic groups with a variety of substitution patterns. These efforts led to an increase in receptor affinity and produced a lactone-based muscarinic ligand with an IC50 of 340nM. As a continuation of that work, additional novel ligands were designed based on the general pharmacophoric elements proposed for the lactone-based ligands. In that model, the lactone oxygens serve as H-bond acceptor moieties while different nitrogen containing heterocycles provide the requisite cationic group. These groups may be separated by linker groups of varying sizes. In order to synthesize the lactone-based ligands mentioned above, efficient synthetic routes are required for key precursors. These include but are not limited to: 1. A novel high yield synthesis of the hydroxyethyl-lactone precursor was designed using a carefully controlled Prins reaction. The method readily quenches a cationic intermediate and simultaneously protects hydroxyl groups in a single step. A mechanism for the new route to the precursor is proposed and its use in the preparation of the target compounds is presented 2. Microwave-assisted synthesis of various sterically hindered N-aryl piperazines has been developed allowing quick access to structurally diverse muscarinic ligands These synthesis along with other newly developed routes enabled ready access to 59 novel muscarinic ligands. The ligands were tested in a general muscarinic binding assay. The result was analyzed and SAR study was performed to direct ligand design. As a result of this work, ligand affinity was improved by over 100 folds compare to the lead molecules. Several promising compounds were selected and selectivity tested.
Temple University--Theses
APA, Harvard, Vancouver, ISO, and other styles
4

Fang, Fang. "Synthesis of Bicyclic and Tricyclic Analogues of Oxazolidinone." Ohio University / OhioLINK, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1357312054.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Nsanzubuhoro, Consolata Nsanzimpaka. "Piperazine-based pyrido[1,2-a]benzimidazoles: synthesis and pharmacological evaluation as potential antimalarial and antischistosomal agents." Master's thesis, Faculty of Science, 2018. http://hdl.handle.net/11427/30112.

Full text
Abstract:
The emergence and spread of parasites resistant to first-line antimalarial drugs comprising artemisinin combination therapies (ACTs) threaten malaria control. There is therefore a need to develop novel and chemically diverse alternatives that are safe, efficacious, and able to circumvent drug resistance. Schistosomiasis is the second most prevalent tropical disease in the world after malaria, and treatment relies on a single drug: praziquantel. Although praziquantel shows multiple benefits over drugs previously used to treat schistosomiasis, dependence on it will result in therapeutic limitations and drug resistance threats. Therefore, there is a dire need to develop novel antischistosomal drugs that are effective and affordable. One attractive approach to accelerate the drug discovery and development process is the exploration of current drugs and drug leads as probable therapies for other diseases. This strategy is known as drug repurposing or drug repositioning, of which the latter is applied in this research project. The cytological similarities in the degradation of haemoglobin performed by Plasmodium parasites and Schistosoma blood flukes in malaria and schistosomiasis, respectively, suggest an opportunity for the repositioning of antimalarial scaffolds as antischistosomal agents. Pyrido[1,2-a]benzimidazoles (PBIs) demonstrate various biological and pharmacological properties such as anti-inflammatory, analgesic, antimicrobial, antiviral, and antineoplastic activities. More recently, PBI derivatives showed favourable in vitro activities against both Plasmodium falciparum and adult Schistosoma mansoni, but modest in vivo potencies. Pharmacokinetic analysis suggests that the sub-optimal in vivo efficacy of PBIs is related to solubility-limited absorption and poor metabolic stability. With the aim of circumventing these challenges, structural modifications have been employed to explore structure-activity and structure-property relationships to produce target compounds with improved druglikeness (Figure A). This study aimed to expand the SAR by performing chemical modifications on the PBI scaffold with the purpose of maintaining or improving biological activity, and to address solubility-limited absorption challenges with this series of compounds (Figure A). The synthesized derivatives were tested against the chloroquine-sensitive (NF54) strain of P. falciparum and against adult S. mansoni concurrently. The most active compound in this PBI series, a di-fluoro-substituted derivative composed of a cyclohexyl piperazine side-chain (33), showed improved in vitro activity against the NF54 strain of P. falciparum (IC50 = 0.012 µM) and enhanced solubility (Figure A). Compounds with methylene or ethylene linkers at the R1 position (Figure A) showed comparable potency, although the directly linked phenyl piperazine analogue showed poor antiplasmodium activity. Compounds containing hydrophobic electron-withdrawing fluoro, chloro, and trifluoromethyl Craig plot substituents at the para position of the phenyl group showed enhanced antiplasmodium activity compared to those containing hydrophobic electron-releasing methyl groups and hydrophilic electron-withdrawing cyano groups. In the LHS-unsubstituted series of compounds, regio-isomerism at substituent R2 (Figure A) resulted in comparable antiplasmodium activity, and this observation was maintained with LHS-substituted PBI derivatives. Notably, unsubstituted derivatives and di-substituted groups displayed moderate to high antiplasmodium potency. Mechanistic evaluations of the compounds revealed non-existent to weak correlations between antiplasmodium activities and their potential to inhibit hemozoin (Hz) formation. This suggests that Hz inhibition is not the sole target of this class of compounds, although it may be a contributory mode of action. Compounds were also screened at 10 µM against newly transformed schistosomula and adult S. mansoni. Two compounds showed high antischistosomal activity against both larval and adult parasites, resulting in > 70% inhibition of worm viability. A turbidimetric assay was carried out to assess the solubility of target PBI compounds. In most cases, the synthesized compounds displayed high in vitro activities and slight improvements in solubility. This therefore encourages further optimization of piperazinyl PBI compounds to improve efficacy and solubility.
APA, Harvard, Vancouver, ISO, and other styles
6

Numa, Mehdi Michel Djamel. "Synthesis of a #NU#, #NU#'-dialkyl piperazine #NU#, #NU#,-dioxide #bait and switch' hapten for proteolytic antibodies." Thesis, University of Nottingham, 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.247571.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Vasconcelos, Leonardo de. "Síntese de um fragmento precursor do fármaco Indinavir." Universidade de São Paulo, 2012. http://www.teses.usp.br/teses/disponiveis/46/46136/tde-23042013-141617/.

Full text
Abstract:
Neste trabalho foram aprofundados nossos estudos para obtenção da (S)-2-terc-butilamida-4-(3-picolil)piperazina, pela abertura da (S)-2-terc-butilcarboxamida-N-p-tosilaziridina seguida de ciclização, em 78% de rendimento, com o triflato de vinildifenilsulfônio. A aziridina foi preparada por um processo de ciclização, em condições de transferência de fase, partindo-se da L-serina, um aminoácido natural de baixo custo. Esta rota sintética rendeu um material que apresenta a mesma estereoquímica S do fragmento piperazínico usado na síntese do Indinavir, podendo vir a constituir uma via alternativa para a obtenção deste fármaco.
In this work we performed a deeper study for obtaining (S)-2-tert-butylamide-4-(3-picolyl)piperazine by opening (S)-2-tert-butylcarboxamide-N-p-tosylaziridine followed by cyclization, in 78% yield, with diphenylvinylsulfonium trifluoromethanesulfonate. The aziridine were prepared by a cyclization process in phase transfer conditions, starting from L-serine, a low cost amino acid. This synthetic route yielded a material which has the same S piperazinic fragment stereochemistry used in the synthesis of Indinavir, and may constitute an alternative route for obtaining this drug.
APA, Harvard, Vancouver, ISO, and other styles
8

Anderson, Laura. "Design and Synthesis of Substituted 1,4-Hydrazine-linked Piperazine-2,5- and 2,6-diones and 2,5-Terpyrimidinylenes as α-Helical Mimetics." Scholar Commons, 2009. https://scholarcommons.usf.edu/etd/1830.

Full text
Abstract:
The most common secondary structure of proteins is the alpha-helix. The alpha-helix can be involved in various protein-protein interactions (PPIs) through the recognition of three or more side chains along one face of the alpha-helix (Wells and McClendon, 2007). In recent years, there has been an increasing interest in the development of peptidic and non-peptidic compounds that bind to PPI surfaces. We focused on the design and synthesis of compounds that mimic the orientation of side chain residues of an alpha-helical protein domain. Although our scaffolds could potentially inhibit various PPIs, we focused mainly on the disruption of interactions among the Bcl-2-family of proteins and the Mdm-2-family of proteins to favor apoptosis in cancer cells. A summary of Bcl-2 and Mdm-2 structure and function relationships that focuses on the possibility of using peptidic and non-peptidic alpha-helical mimics as PPI inhibitors is described in Chapter One. Chapter Two discusses the design and synthesis of 3-substituted-2,6- and 2,5-piperazinedione oligomers as more hydrophilic scaffolds compared to previously reported alpha-helical mimetics (Yin, et al., 2005). A key feature of this design is the linkage of the units by a hydrazine bond. While we were able to prepare several monomers containing the hydrazine linkage, synthesis of the dimers and trimers is very challenging. Due to the difficulty of synthesizing oligomeric piperazine-diones in practical yields, we next focused on the design and synthesis of novel 2,5-terpyrimidinylene scaffolds as an alternative to obtain alpha-helical mimetics; this is discussed in Chapter Three. The main outcome of this project was the efficient preparation of a "first-generation" non-peptidic compound library via a facile iterative synthesis enabled by the key conversion of 5-cyanopyrimidine to 5-carboxamidine. Chapter Three also discusses our progress towards the synthesis of structurally similar substituted-2,5-terpyrimidinylenes, but with more drug-like properties as determined by QikProp calculations. Chapter Four describes an independent study on the synthesis of a guanidine derivative as an alkylating agent for the synthesis of cysteine peptide nucleic acids, CPNA, which is another current project in our lab.
APA, Harvard, Vancouver, ISO, and other styles
9

Andersson, Hans. "Reaction between grignard reagents and heterocyclic N-oxides synthesis of substituted pyridines, piperidines and piperazines /." Doctoral thesis, Umeå : Department of Chemistry, Umeå University, 2009. http://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-25619.

Full text
APA, Harvard, Vancouver, ISO, and other styles
10

Monaghan, S. M. "Synthetic studies in the piperazine-2,5-dione area." Thesis, Imperial College London, 1987. http://hdl.handle.net/10044/1/47304.

Full text
APA, Harvard, Vancouver, ISO, and other styles
More sources

Book chapters on the topic "Piperazine Synthesis"

1

Huang, Yijun, Kareem Khoury, and Alexander Dömling. "The Piperazine Space in Isocyanide-based MCR Chemistry." In Synthesis of Heterocycles via Multicomponent Reactions I, 85–127. Berlin, Heidelberg: Springer Berlin Heidelberg, 2010. http://dx.doi.org/10.1007/7081_2010_27.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Yamamoto, Koki. "Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Synthesis and Application of Fused Piperazine Derivatives for Investigation of Degradable Core Motifs." In Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists, 27–70. Singapore: Springer Singapore, 2020. http://dx.doi.org/10.1007/978-981-15-2965-8_3.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Handy, Emma L., and Jason K. Sello. "Structure and Synthesis of Conformationally Constrained Molecules Containing Piperazic Acid." In Topics in Heterocyclic Chemistry, 97–124. Cham: Springer International Publishing, 2015. http://dx.doi.org/10.1007/7081_2015_185.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Ye, Z. S. "40.1.8 Product Subclass 8: Piperazines." In Knowledge Updates 2021/2. Stuttgart: Georg Thieme Verlag KG, 2021. http://dx.doi.org/10.1055/sos-sd-140-00314.

Full text
Abstract:
AbstractThe piperazine unit is widely distributed in natural products and life-saving small-molecule pharmaceuticals. It is the third most common nitrogen heterocycle occurring in pharmaceuticals approved by the U. S. Food and Drug Administration. This chapter covers strategies for the synthesis and transformations of piperazines, with both classical methods and recent developments reviewed. A major focus is on cyclization reactions such as intramolecular hydroaminations, multicomponent approaches, and routes from ethane-1,2-diamine substrates. Also discussed are approaches based on hydrogenation of (hydro)pyrazines by heterogeneous catalysis and by (asymmetric) homogeneous catalysis. Finally, a variety of transformations involving modification of a substituent on a piperazine ring are surveyed, including arylations, alkylations, and oxidations.
APA, Harvard, Vancouver, ISO, and other styles
5

Avendaño, Carmen, and Elena de la Cuesta. "Synthetic Chemistry with N-Acyliminium Ions derived from Piperazine-2,5-diones and Related Compounds." In Advances in Organic Synthesis, 309–54. BENTHAM SCIENCE PUBLISHERS, 2013. http://dx.doi.org/10.2174/9781608054800113050009.

Full text
APA, Harvard, Vancouver, ISO, and other styles
6

Weitkamp, J., S. Ernst, H. J. Buysch, and D. Lindner. "Synthesis of Piperazine and Triethylenediamine Using Zsm-5-Type Zeolite Catalysts." In Studies in Surface Science and Catalysis, 297–304. Elsevier, 1991. http://dx.doi.org/10.1016/s0167-2991(08)62914-6.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Unger, Thomas A. "Piperazines." In Pesticide Synthesis Handbook, 495. Elsevier, 1996. http://dx.doi.org/10.1016/b978-081551401-5.50388-9.

Full text
APA, Harvard, Vancouver, ISO, and other styles
8

Hendrix, James A., David Stefany, Sarah L. Brooks, George E. Lee, Jean-François Sabuco, Eric MacMillan, Leila Albers, Shelley Pavlek, Nicola Collar, and Ephraim Vidal. "The Synthesis of Novel Thienoisoxazole Piperidines and Thienopyrazole Piperazines." In 19th International Congress on Heterocyclic Chemistry, 170. Elsevier, 2003. http://dx.doi.org/10.1016/b978-0-08-044304-1.50162-3.

Full text
APA, Harvard, Vancouver, ISO, and other styles

Conference papers on the topic "Piperazine Synthesis"

1

Loupias, Pauline, Alexandra Dassonville-Klimpt, Elodie Lohou, Nicolas Taudon, and Pascal Sonnet. "Trojan horse strategy: synthesis of piperazine-based siderophores." In 4th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2018. http://dx.doi.org/10.3390/ecmc-4-05579.

Full text
APA, Harvard, Vancouver, ISO, and other styles
2

Pazdera, P., B. Andělová, and D. Němečková. "Utilization of piperazine for interphase catalytic systems." In The 13th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2009. http://dx.doi.org/10.3390/ecsoc-13-00192.

Full text
APA, Harvard, Vancouver, ISO, and other styles
3

Corredoira-Vázquez, Julio, Paula Oreiro-Martínez, Ana M. García Deibe, Jesús Sanmartín-Matalobos, and Matilde Fondo. "Rearrangement of Imidazolidine to Piperazine Rings in the Presence of DyIII." In International Electronic Conference on Synthetic Organic Chemistry. Basel Switzerland: MDPI, 2022. http://dx.doi.org/10.3390/ecsoc-26-13547.

Full text
APA, Harvard, Vancouver, ISO, and other styles
4

Li, Heping, and Zhoudong Wang. "Synthesis of Lactosylated Piperazinyl Porphyrin and its Interaction with DNA." In 2008 2nd International Conference on Bioinformatics and Biomedical Engineering. IEEE, 2008. http://dx.doi.org/10.1109/icbbe.2008.34.

Full text
APA, Harvard, Vancouver, ISO, and other styles
5

Sevcik, Richard, Dana Němečková, Eva Havránková, Jan Šimbera, and Pavel Pazdera. "Sophisticated synthesis of monosubstituted piperazines – from a batch reaction vessel to a flow (microwave) reactor." In The 23rd International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecsoc-23-06478.

Full text
APA, Harvard, Vancouver, ISO, and other styles
6

Recabarren-Gajardo, G., C. Espinosa-Bustos, D. Hebel, W. Meza, F. Tapia, A. Zárate, C. F. Lagos, and C. D. Pessoa-Mahana. "Design and Synthesis of 3-[1-oxo-(4-aryl-1-piperazinyl)alkyl]-N- (arylsulfonyl)-indoles as Potential Antagonists Agents on 5- HT6 Receptors." In 14th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0169-2.

Full text
APA, Harvard, Vancouver, ISO, and other styles
7

Andrić, Deana B., Slađana Dukić-Stefanovic, Jelena Z. Penjišević, Ivana I. Jevtić, Vladimir B. Šukalović, Relja Suručić, and Slađana Kostić-Rajačić. "DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL N- {4-[2-(4-ARYL-PIPERAZIN-1-YL)-ETHYL]-PHENYL}-ARYLAMIDES." In 1st INTERNATIONAL Conference on Chemo and BioInformatics. Institute for Information Technologies, University of Kragujevac, 2021. http://dx.doi.org/10.46793/iccbi21.355a.

Full text
Abstract:
5HT1A receptor targeting drugs have been used as the treatment for the many neuropsychiatric disorders, such as schizophrenia and depression. As a part of ongoing research, we designed series of new compounds that share arylpiperazine common structural motif with the 5HT1A receptor ligand aripiprazole. Receptor-ligand interactions were determined by the molecular docking simulations, revealing the positive impact of the phenyl substitution in the arylpiperazine part of the molecules. Nine selected compounds were synthesized in four reaction steps in high overall yields (59-73%). In vitro pharmacological evaluation of the synthesized compounds revealed three compounds (5b, 6b and 6c) with high 5HT1A binding affinity, comparable with aripiprazole (Ki 12.0, 4.8, 12.8, 5.6 nM, respectively). Compounds from b series, 5b and 6b, possess 2-methoxyphenyl substituents, while 6c possess 2,3-dichlorophenyl substituent in the arylpiperazine part of the molecule. The pharmacological results are therefore in accordance with the molecular docking simulations thus proving the rational design. Compounds 5c, 6b and 6c can be considered as the candidates for further evaluation as new, potential antidepressants.
APA, Harvard, Vancouver, ISO, and other styles
8

Renk, D., M. Holschbach, D. Bier, and B. Neumaier. "Synthese von Aminobenzothiazolderivaten mit unterschiedlichen fluorhaltigen Piperidin- und Piperazin-Substituenten für die PET-Bildgebung des Adenosin-A 2A -Rezeptors." In NuklearMedizin 2020. © Georg Thieme Verlag KG, 2020. http://dx.doi.org/10.1055/s-0040-1708273.

Full text
APA, Harvard, Vancouver, ISO, and other styles
9

Ananth, Arjun H., and Senthamaraikannan Kabilan. "Synthesis, In Silico and In Vitro Studies of 7-Methxy-3-((4-phenyl piperazin-1-yl)methyl)-2H-chromen-2-one Analogues as Derivatives as Anti-Prostate Cancer Agents." In ECMC 2022. Basel Switzerland: MDPI, 2022. http://dx.doi.org/10.3390/ecmc2022-13179.

Full text
APA, Harvard, Vancouver, ISO, and other styles
You might also be interested in the extended bibliographies on the topic 'Piperazine Synthesis' for particular source types:
Journal articles Dissertations / Theses
We offer discounts on all premium plans for authors whose works are included in thematic literature selections. Contact us to get a unique promo code!

To the bibliography