Academic literature on the topic 'Piperazine Synthesis'

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Journal articles on the topic "Piperazine Synthesis"

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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.

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

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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 Cycliz
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Hafeez, Freeha, Ameer Fawad Zahoor, Azhar Rasul, et al. "Ultrasound-Assisted Synthesis and In Silico Modeling of Methanesulfonyl-Piperazine-Based Dithiocarbamates as Potential Anticancer, Thrombolytic, and Hemolytic Structural Motifs." Molecules 27, no. 15 (2022): 4776. http://dx.doi.org/10.3390/molecules27154776.

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

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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
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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.

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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
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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 (2016): 42–55. http://dx.doi.org/10.2174/1874842201603010042.

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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-
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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 (2014): 838–48. http://dx.doi.org/10.1139/cjc-2014-0242.

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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 [
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Penjisevic, Jelena, Vladimir Sukalovic, Deana Andric, et al. "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.

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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.
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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.

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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
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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.

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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.
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Dissertations / Theses on the topic "Piperazine Synthesis"

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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.

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

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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 chemic
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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.

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Pharmaceutical Sciences<br>Ph.D.<br>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 in
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Fang, Fang. "Synthesis of Bicyclic and Tricyclic Analogues of Oxazolidinone." Ohio University / OhioLINK, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1357312054.

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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.

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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 limitati
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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.

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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/.

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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
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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.

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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 PP
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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.

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

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Book chapters on the topic "Piperazine Synthesis"

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

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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. Springer Singapore, 2020. http://dx.doi.org/10.1007/978-981-15-2965-8_3.

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

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

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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.
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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. BENTHAM SCIENCE PUBLISHERS, 2013. http://dx.doi.org/10.2174/9781608054800113050009.

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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. Elsevier, 1991. http://dx.doi.org/10.1016/s0167-2991(08)62914-6.

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

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Hendrix, James A., David Stefany, Sarah L. Brooks, et al. "The Synthesis of Novel Thienoisoxazole Piperidines and Thienopyrazole Piperazines." In 19th International Congress on Heterocyclic Chemistry. Elsevier, 2003. http://dx.doi.org/10.1016/b978-0-08-044304-1.50162-3.

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Conference papers on the topic "Piperazine Synthesis"

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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. MDPI, 2018. http://dx.doi.org/10.3390/ecmc-4-05579.

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

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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. MDPI, 2022. http://dx.doi.org/10.3390/ecsoc-26-13547.

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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.

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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. MDPI, 2019. http://dx.doi.org/10.3390/ecsoc-23-06478.

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Recabarren-Gajardo, G., C. Espinosa-Bustos, D. Hebel, et al. "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. Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0169-2.

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Andrić, Deana B., Slađana Dukić-Stefanovic, Jelena Z. Penjišević, et al. "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.

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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 pharm
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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.

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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. MDPI, 2022. http://dx.doi.org/10.3390/ecmc2022-13179.

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