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Journal articles on the topic 'Piperazino'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

Vejdělek, Zdeněk, and Miroslav Protiva. "N-(piperazinoacyl) and N-(piperazinoalkyl) derivatives of 4-cyclopentylaniline and related compounds: Synthesis and pharmacological screening." Collection of Czechoslovak Chemical Communications 51, no. 7 (1986): 1494–502. http://dx.doi.org/10.1135/cccc19861494.

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Five N-(4-cyclopentylphenyl)haloalkanecarboxamides were reacted with 1-methylpiperazine and 1-(2-hydroxyethyl)piperazine to give the corresponding N-(4-cyclopentylphenyl)piperazinoalkanecarboxamides Iab -Vab. Their reduction with lithium aluminium hydride afforded the triamines VIIab - XIab. Acylation of the N-(4-methylpiperazino)alkyl-4-cyclopentylanilines Xa and XIa with propionyl chloride resulted in the propionanilides XIVa and XVa, whereas a similar reaction of the N-(4-(2-hydroxyethyl)piperazino)alkyl-4-cyclopentylanilines VIIb and IXb - XIb produced the propionoxypropionanilides XIIc -

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2

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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3

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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4

Jílek, Jiří, Jiří Holubek, Emil Svátek, et al. "Potential metabolites of the neuroleptic agents belonging to the 8-methylthio-10-piperazino-10,11-dihydrodibenzo[b,f]thiepin series; Synthesis of 2-hydroxy and 3-hydroxy derivatives." Collection of Czechoslovak Chemical Communications 50, no. 10 (1985): 2179–90. http://dx.doi.org/10.1135/cccc19852179.

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The acid VI, prepared by reaction of potassium salts of (2-iodo-5-methoxyphenyl)acetic acid and 4-(methylthio)thiophenol in the presence of copper, was transformed via intermediates VII-IX to 2-methoxy-8-methylthio-10-piperazino-10,11-dihydrodibenzo[b,f]thiepins X and XI. Their demethylation with boron tribromide afforded 2-hydroxy derivatives of the neuroleptic agents methiothepin and oxyprothepin I and II. 11-Chloro-7-methoxy-2-methylthio-10,11-dihydrodibenzo[b,f]thiepin was subjected to substitution reactions with 1-methylpiperazine and 1-(ethoxycarbonyl)piperazine and gave piperazine deriv

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5

Lawson, Edward C., Diane K. Luci, Shyamali Ghosh, et al. "Nonpeptide Urotensin-II Receptor Antagonists: A New Ligand Class Based on Piperazino-Phthalimide and Piperazino-Isoindolinone Subunits." Journal of Medicinal Chemistry 52, no. 23 (2009): 7432–45. http://dx.doi.org/10.1021/jm900683d.

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6

Lou, Chenguang, Birte Vester, and Jesper Wengel. "Oligonucleotides containing a piperazino-modified 2′-amino-LNA monomer exhibit very high duplex stability and remarkable nuclease resistance." Chemical Communications 51, no. 19 (2015): 4024–27. http://dx.doi.org/10.1039/c5cc00322a.

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Incorporation of a novel piperazino-modified 2′-amino-LNA monomer (PipLNA-T) into oligonucleotides leads to a pronounced affinity increase against complementary DNA and RNA and a strong stabilising effect against 3′-exonucleolytic degradation.

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7

Pandey, Anubhuti, Sarvesh Kumar Paliwal, and Shailendra Kumar Paliwal. "Chemical Feature-Based Molecular Modeling of Urotensin-II Receptor Antagonists: Generation of Predictive Pharmacophore Model for Early Drug Discovery." Journal of Chemistry 2014 (2014): 1–16. http://dx.doi.org/10.1155/2014/921863.

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For a series of 35 piperazino-phthalimide and piperazino-isoindolinone based urotensin-II receptor (UT) antagonists, a thoroughly validated 3D pharmacophore model has been developed, consisting of four chemical features: one hydrogen bond acceptor lipid (HBA_L), one hydrophobe (HY), and two ring aromatic (RA). Multiple validation techniques like CatScramble, test set prediction, and mapping analysis of advanced known antagonists have been employed to check the predictive power and robustness of the developed model. The results demonstrate that the best model, Hypo 1, shows a correlation (r) of

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8

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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9

Desai, Akshay D., and Kishor H. Chikhalia. "Synthesis and Studies of 1-[2-(Aryl Amino-2-Oxo Ethyl) Amino]-4-(N-Methyl Piperazino)-Benzene Derivatives." E-Journal of Chemistry 2, no. 1 (2005): 15–20. http://dx.doi.org/10.1155/2005/575290.

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1-[2-(Aryl Amino-2-Oxo Ethyl) Amino]-4-(N-Methyl Piperazino)-Benzene Derivatives were synthesized. The synthesized compounds were screened for their antibacterial activities againstS.auresandE.coliby cup plat method. From screening result some compounds found highly active against both Gram-positive and Gram-negative bacteria while other compounds possess feeble to moderate activity.

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10

Bogeso, Klaus P., Jorn Arnt, Kristen Frederiksen, Hans Otto Hansen, John Hyttel, and Henrik Pedersen. "Enhanced D1 Affinity in a Series of Piperazine Ring Substituted 1-Piperazino-3-Arylindans with Potential Atypical Antipsychotic Activity." Journal of Medicinal Chemistry 38, no. 22 (1995): 4380–92. http://dx.doi.org/10.1021/jm00022a004.

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11

Gendugov, T. A., A. A. Glushko, A. A. Ozerov та L. I. Shcherbakova. "STUDY OF THE STABILITY OF THE SUBSTANCE 3-[2-(4-PHENYL-1-PIPERAZINO)-2-OXOETHYL]QUINAZOLINE-4(3Н)-ONE UNDER STRESSFUL CONDITIONS". Pharmacy & Pharmacology 8, № 4 (2021): 242–54. http://dx.doi.org/10.19163/2307-9266-2020-8-4-242-254.

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The aim of the research was to study the stability of a new pharmaceutical substance 3-[2-(4-phenyl-1-piperazino)-2-oxoethyl]quinazoline-4(3Н)-one under stress conditions.Materials and methods. The study was conducted in accordance with the recommendations of the ICH guidelines. The object of the study was a previously unknown derivative of quinazoline-4(3H)-one: 3-[2-(4-phenyl-1-piperazino)-2-oxoethyl] quinazoline-4(3Н)-one synthesized in Volgograd state medical university. The following laboratory equipment was used: HPLC chromatograph, HPLC-MS, centrifuge, electronic scales, pH meter, therm

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12

Verma, Arvind Kumar, Arun Kumar, and Kunwar Abhishek Singh. "Synthesis and molecular docking for anticonvulsant activity of some new benzoxazole derivatives." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 02 (2025): 551. https://doi.org/10.59467/ijhc.2025.35.551.

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To explore the anticonvulsant action related to the benzoxazole framework, a series of benzoxazole-piperazine derivatives, namely N-(4-(benzo[d]oxazol-2-yl)phenyl)-2-(piperazin-1-yl) acetamides (3a-e) (3), was synthesized by reacting N-(4-(benzo[d]oxazol-2-yl)phenyl)-2-chloroacetamide (2) with various substituted piperazines. Molecular docking studies were conducted using Auto Dock Vina 1.5.7 to evaluate the compounds' binding affinities with anticonvulsant-related targets protein data bank ID: 3PO7, 7WLJ, using zonisamide as a standard drug to ensure their potential. Several compounds exhibit

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13

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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14

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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15

Waisser, Karel, and Jana Bořková. "Relations between structure and antituberculotic activity in a group of 10-piperazino-10,11-dihydrodibenzo[b,f]thiepins." Collection of Czechoslovak Chemical Communications 56, no. 11 (1991): 2395–401. http://dx.doi.org/10.1135/cccc19912395.

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Relations between chemical structure and activity to Mycobacterium tuberculosis have been looked for within a group of the derivatives of 10-piperazino-10,11-dihydrodibenzo[b,f]thiepins prepared by Protiva et al. It has been found that the most reliable results are obtained with application of the model by Free and Wilson. The activity can be considered additive with regard to the contributions of the molecular segments varied.

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16

N., Kalarani, Angumeenal AR., Kamalakannan P., and Venkappayya D. "Synthesis and characterization of piperazino-bis(methylantipyrine) and its complexes with chromium(III), manganese(II), cobalt(II), copper(II), zinc(II) and cadmium(II) ions." Journal of Indian Chemical Society Vol. 82, May 2005 (2005): 404–10. https://doi.org/10.5281/zenodo.5829979.

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Department of Chemistry, National Institute or Technology, Tiruchirappalli-620 015, India School of Chemical and Biotechnology, SASTRA Deemed University, Thanjavur-613 402. India <em>E-mail</em> : angum@nitt.edu <em>Manuscript received 3 September 2003, revised 23 June 2004, accepted 2 February 2005</em> A new Mannich base, piperazino-his(methylantipyrine) (PBMA), was synthesized and characterized by spectral studies. Chelates of PBMA with chromium(III), manganese(ll), cobalt(II), copper(II), zinc(II) and cadmium(II) ions were prepared and characterized by elemental analyses and IR, UV and <su

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17

Berezhnaya, V. N., R. P. Shishkina, and E. P. Fokin. "Thermal conversions of 2-azido-3-piperazino-substituted 1,4-naphthoquinones." Bulletin of the Academy of Sciences of the USSR Division of Chemical Science 37, no. 12 (1988): 2545–49. http://dx.doi.org/10.1007/bf00952637.

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18

Janaswamy, Srinivas, G. Sreenivasa Murthy, T. Mohan, and M. N. Sudheendra Rao. "Crystal structure analysis of (N-methyl piperazino) (phenyl) (dicyclohexylamino) phosphiniminocyclotrithiazene." Journal of Chemical Crystallography 35, no. 1 (2005): 27–34. http://dx.doi.org/10.1007/s10870-005-1150-y.

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19

Jílek, Jiří, Martin Valchář, Josef Pomykáček, Antonín Dlabač, and Miroslav Protiva. "Noncataleptic neuroleptic agents: Synthesis of some esters of 2-chloro-10-(4-(2-hydroxyethyl)piperazino)-10,11-dihydrodibenzo[b,f]thiepin." Collection of Czechoslovak Chemical Communications 51, no. 7 (1986): 1503–8. http://dx.doi.org/10.1135/cccc19861503.

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Reactions of 2-chloro-10-(4-(2-hydroxyethyl)piperazino)-10,11-dihydrodibenzo[b,f]thiepin (I) with phenylacetic, methoxyacetic, methylthioacetic, phenoxyacetic and morpholinoacetic acid in dichloromethane and in the presence of N,N'-carbonyldiimidazole gave the title esters II - VI. Reaction of I with succinic anhydride afforded the hemisuccinate VII. The esters prepared elicited ataxia in low doses, were low-cataleptic, but only II, IV, and VII proved some antidopaminergic activity in the test using the affecting dopamine metabolism in rat brain striatum.

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20

Lindstaedt, Agnieszka, Justyna Doroszuk, Aneta Machnikowska, et al. "Effects Induced by the Temperature and Chemical Environment on the Fluorescence of Water-Soluble Gold Nanoparticles Functionalized with a Perylene-Derivative Dye." Materials 17, no. 5 (2024): 1097. http://dx.doi.org/10.3390/ma17051097.

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We developed a fluorescent molecular probe based on gold nanoparticles functionalized with N,N′-bis(2-(1-piperazino)ethyl)-3,4,9,10-perylenetetracarboxylic acid diimide dihydrochloride, and these probes exhibit potential for applications in microscopic thermometry. The intensity of fluorescence was affected by changes in temperature. Chemical environments, such as different buffers with the same pH, also resulted in different fluorescence intensities. Due to the fluorescence intensity changes exhibited by modified gold nanoparticles, these materials are promising candidates for future technolo

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21

BOEGESOE, K. P., J. ARNT, K. FREDERIKSEN, H. O. HANSEN, J. HYTTEL, and H. PEDERSEN. "ChemInform Abstract: Enhanced D1 Affinity in a Series of Piperazine Ring Substituted 1- Piperazino-3-arylindans with Potential Atypical Antipsychotic Activity." ChemInform 27, no. 10 (2010): no. http://dx.doi.org/10.1002/chin.199610213.

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22

Jílek, Jiří, Martin Valchář, Jiří Holubek, et al. "Noncataleptic neuroleptic agents: 2-(4-(2-(2-Chloro-10,11-dihydrodibenzo[b,f]thiepin-10-yloxy)ethyl)piperazine-1-yl)ethanol and some related compounds." Collection of Czechoslovak Chemical Communications 53, no. 11 (1988): 2731–41. http://dx.doi.org/10.1135/cccc19882731.

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10-(2-Bromoethoxy)-2-chloro-10,11-dihydrodibenzo[b,f]thiepin (X), prepared by two methods, was subjected to substitution reactions with 2-(1-piperazinyl)ethanol, 3-(1-piperazinyl)propanol, 1-methylpiperazine, 3-(1-piperazinyl)propionamide, piperazine, and 1-(ethoxycarbonyl)piperazine and gave the title compounds II-VII. The alcohol II was esterified by treatment with acid chlorides to compounds VIII and IX. Compounds II, V, and VIII proved to be noncataleptic neuroleptic agents and II (clopithepin, VÚFB-17 076) was selected for preclinical studies.

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23

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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24

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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25

Spencer, John, Andrew P. Burd, Christopher A. Goodwin, et al. "Synthesis of ortho-modified mercapto- and piperazino-methyl-phenylboronic acid derivatives." Tetrahedron 58, no. 8 (2002): 1551–56. http://dx.doi.org/10.1016/s0040-4020(01)01028-6.

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26

Song, Yanxi, C. S. Chidan Kumar, G. B. Nethravathi, S. Naveen, and Hongqi Li. "Cinnarizinium picrate." Acta Crystallographica Section E Structure Reports Online 68, no. 6 (2012): o1747. http://dx.doi.org/10.1107/s1600536812020764.

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In the title salt {systematic name: 4-diphenylmethyl-1-[(E)-3-phenylprop-2-en-1-yl]piperazin-1-ium 2,4,6-trinitrophenolate), C26H29N2 +·C6H2N3O7 −, the cinnarizinium cation is protonated at the piperazine N atom connected to the styrenylmethyl group; the piperazine ring adopts a distorted chair conformaiton. In the crystal, bifurcated N—H...(O,O) hydrogen bonds link the components into two-ion aggregates.

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27

Gauci, Gabriel, and David C. Magri. "Solvent-polarity reconfigurable fluorescent 4-piperazino-N-aryl-1,8-naphthalimide crown ether logic gates." RSC Advances 12, no. 54 (2022): 35270–78. http://dx.doi.org/10.1039/d2ra07568g.

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28

Nivedita Desai, R., S. Sreenivasa, S. Naveen, N. K. Lokanath, P. A. Suchetan, and D. B. Aruna Kumar. "Crystal structure of 2-(4-methylpiperazin-1-yl)quinoline-3-carbaldehyde." Acta Crystallographica Section E Crystallographic Communications 71, no. 11 (2015): o900—o901. http://dx.doi.org/10.1107/s2056989015020186.

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In the title compound, C15H17N3O, the aldehyde group is twisted relative to the quinoline group by17.6 (2)° due to the presence of a bulky piperazinyl group in theorthoposition. The piperazine N atom attached to the aromatic ring issp3-hybridized and the dihedral angle between the mean planes through the the six piperazine ring atoms and through the quinoline ring system is 40.59 (7)°. Both piperazine substituents are in equatorial positions.

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29

Wilson, W. David, Henryk J. Barton, Farial A. Tanious, Suk-Bin Kong, and Lucjan Strekowski. "The interaction with DNA of unfused aromatic systems containing terminal piperazino substituents." Biophysical Chemistry 35, no. 2-3 (1990): 227–43. http://dx.doi.org/10.1016/0301-4622(90)80011-u.

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30

Sirakanyan, S. N., É. K. Akopyan, R. G. Paronikyan, I. M. Nazaryan, A. G. Akopyan, and A. A. Ovakimyan. "Synthesis and Neurotropic Activity of Piperazino-Derivatives of Pyrano[3,4-c]Pyridines." Pharmaceutical Chemistry Journal 53, no. 6 (2019): 495–99. http://dx.doi.org/10.1007/s11094-019-02026-8.

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31

Szollosi, Doreen E., Ola A. M. Ghoneim, Mohammed K. Manzoor, Jyothi Dhuguru, and Ivan O. Edafiogho. "Novel Piperazino-Enaminones Suppress Pro-Inflammatory Cytokines and Inhibit Chemokine Receptor CCR2." Inflammation 39, no. 6 (2016): 2053–61. http://dx.doi.org/10.1007/s10753-016-0443-y.

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32

Billard, Thierry, Bernard R. Langlois, and Gaëlle Blond. "Trifluoromethylation of Nonenolizable Carbonyl Compounds with a Stable Piperazino Hemiaminal of Trifluoroacetaldehyde." European Journal of Organic Chemistry 2001, no. 8 (2001): 1467–71. http://dx.doi.org/10.1002/1099-0690(200104)2001:8<1467::aid-ejoc1467>3.0.co;2-a.

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33

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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34

Prabawati, Susy Yunita. "SYNTHESIS OF 1,4-BIS [(1-HYDROXY-4-T-BUTYL-PHENYL) METHYL]PIPERAZINE AS ANTIOXIDANTS." Molekul 11, no. 2 (2016): 220. http://dx.doi.org/10.20884/1.jm.2016.11.2.244.

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A study has been conducted to synthesize 1,4-bis [(1-hydroxy-4-t-butyl-phenyl)-methyl]piperazin using phenol derivate and investigate the capability of that compound, as an antioxidant. The synthesis was carried out through Mannich reaction using p-t-butylphenol, paraformaldehyde, and piperazine. The product was characterized by IR and 1H NMR spectroscopic. Testing of antioxidant activity was done with the immersion of DPPH (1,1-diphenyl-2 picrylhydrazyl) free radical method. The product was obtained as a white solid, with a point of 252,7-254,7 ºC and a yield of 65.76%. The test of antioxidan

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35

Mosca, Alessio, Stefania Chiappini, Andrea Miuli, et al. "Piperazine Abuse and Psychosis: A Systematic Review of the Literature." Psychiatry International 5, no. 3 (2024): 552–63. http://dx.doi.org/10.3390/psychiatryint5030040.

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Background: Piperazines, synthetic compounds known for their stimulant and hallucinogenic effects, have gained prominence among novel psychoactive substances (NPS) and are frequently associated with adverse psychiatric outcomes, including psychosis. Methods: A systematic review of the literature available up to 23 May 2024 was conducted, using the PubMed, Scopus, and Web of Science databases, in addition to the related gray literature, utilizing the following search strategy: “piperazines” AND (“psychosis” OR “hallucination” OR “delusion” OR “schizophrenia” OR “delusional” OR “schizoaffective”

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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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Erdag, Emine. "A New Tick on the Clock: Indole-Based Optimization of Melatonin Receptor Modulators." Chronobiology in Medicine 7, no. 2 (2025): 88–94. https://doi.org/10.33069/cim.2025.0014.

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Objective: Melatonin is a key regulator of circadian rhythms and sleep-wake cycles, exerting its effects through MT1 and MT2 receptors. Despite the clinical use of selective MT1/MT2 agonists, their short half-lives, low bioavailabilities, and rapid first-pass metabolism limit their efficacy in sleep and circadian rhythm disorders. This study aimed to identify and evaluate novel piperazine-substituted indole derivatives with enhanced receptor binding, prolonged systemic circulation, and improved pharmacokinetic properties as potential next-generation melatonin receptor modulators.Methods: Seven

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Al-Soud, Yaseen, Najim Al-Masoudi, Hamed Hassan, Erik De Clercq, and Christophe Pannecouque. "Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives." Acta Pharmaceutica 57, no. 4 (2007): 379–93. http://dx.doi.org/10.2478/v10007-007-0031-7.

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Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivativesA series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H- -imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and alkyl- [4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin- -1-yl)ketones (11-20) as well as the indole analogue22were synthesized from 4-nitro-5-piperazinyl imidazole derivative1, with the aim to develop newly non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound2showed i

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Periasamy, Mariappan, Boda Venkanna, Miriyala Nagaraju, and Lakavathu Mohan. "Methods for the Synthesis of Piperazine Derivatives Containing a Chiral Bi-2-naphthyl Moiety." Synthesis 52, no. 01 (2019): 127–34. http://dx.doi.org/10.1055/s-0037-1610731.

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Piperazine derivatives containing 1,1′-bi-2-naphthyl moiety were synthesized starting from 2,2′-dimethoxy-1,1′-bi-naphthalene via acylation using ethyl chlorooxoacetate and subsequent condensation with 1,2-diamines followed by reduction of the corresponding dihydro-2-piperazinone intermediate using the NaBH4/I2 reagent system. The corresponding chiral piperazine derivatives containing bi-2-napthyl moiety was synthesized by asymmetric reduction of ethyl dimethoxy-bi-2-naphthyloxoacetate by chiral oxazoborolidine catalyst prepared in situ using S-diphenylprolinol (S-DPP), B(OCH3)3 and H3B·THF. T

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Rayala, Ramanjaneyulu, Prakash Chaudhari, Ashley Bunnell, Bracken Roberts, Debopam Chakrabarti, and Adel Nefzi. "Parallel Synthesis of Piperazine Tethered Thiazole Compounds with Antiplasmodial Activity." International Journal of Molecular Sciences 24, no. 24 (2023): 17414. http://dx.doi.org/10.3390/ijms242417414.

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Thiazole and piperazine are two important heterocyclic rings that play a prominent role in nature and have a broad range of applications in agricultural and medicinal chemistry. Herein, we report the parallel synthesis of a library of diverse piperazine-tethered thiazole compounds. The reaction of piperazine with newly generated 4-chloromethyl-2-amino thiazoles led to the desired piperazine thiazole compounds with high purities and good overall yields. Using a variety of commercially available carboxylic acids, the parallel synthesis of a variety of disubstituted 4-(piperazin-1-ylmethyl)thiazo

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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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Stöver, Harald D. H., and Christian Detellier. "Structural identification of a new piperazino-crown ether derivative using 23Na nuclear magnetic resonance." Tetrahedron Letters 30, no. 33 (1989): 4333–36. http://dx.doi.org/10.1016/s0040-4039(00)99353-5.

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Sirakanyan, S. N., A. S. Noravyan, I. A. Dzhagatspanyan, et al. "Synthesis and neurotropic activity of new derivatives of piperazino-substituted pyrano[3,4-c]pyridines." Pharmaceutical Chemistry Journal 46, no. 10 (2013): 591–94. http://dx.doi.org/10.1007/s11094-013-0852-2.

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Zhong, Chen, Doreen Szollosi, Junjiang Sun, et al. "Novel Piperazino-Enaminones Decrease Pro-inflammatory Cytokines Following Hemarthrosis in a Hemophilia Mouse Model." Inflammation 42, no. 5 (2019): 1719–29. http://dx.doi.org/10.1007/s10753-019-01032-y.

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Bøgesø, Klaus P., and Michael Bech Sommer. "The effect of aromatic substitution on neuroleptic activity in 1-piperazino-3-phenylindans. A comparison based on a new D-2 receptor model with corresponding 10-piperazino-10,11-dihydrodibenzo[b,f]thiepins." Collection of Czechoslovak Chemical Communications 56, no. 11 (1991): 2456–67. http://dx.doi.org/10.1135/cccc19912456.

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The validity of a new dopamine D-2 receptor interaction model based on conformational analysis and least-squares superimposition studies of the indan derivative tefludazine and the thiepin derivative octoclothepin was further tested by comparison of the effect of aromatic substitution on D-2 antagonistic activity in two series of indan and thiepin derivatives. The indan series include new derivatives substituted in the 4-, 7-, 2’- and 3’-position. The substitution effects were largely parallel with one important exception: Only 6-substituted indans have significant neuroleptic activity while b

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Kiran Kumar, Haruvegowda, Hemmige S. Yathirajan, Belakavadi K. Sagar, Sabine Foro, and Christopher Glidewell. "Six 1-aroyl-4-(4-methoxyphenyl)piperazines: similar molecular structures but different patterns of supramolecular assembly." Acta Crystallographica Section E Crystallographic Communications 75, no. 8 (2019): 1253–60. http://dx.doi.org/10.1107/s2056989019010491.

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Six new 1-aroyl-4-(4-methoxyphenyl)piperazines have been prepared, using coupling reactions between benzoic acids and N-(4-methoxyphenyl)piperazine. There are no significant hydrogen bonds in the structure of 1-benzoyl-4-(4-methoxyphenyl)piperazine, C18H20N2O2, (I). The molecules of 1-(2-fluorobenzoyl)-4-(4-methoxyphenyl)piperazine, C18H19FN2O2, (II), are linked by two C—H...O hydrogen bonds to form chains of rings, which are linked into sheets by an aromatic π–π stacking interaction. 1-(2-Chlorobenzoyl)-4-(4-methoxyphenyl)piperazine, C18H19ClN2O2, (III), 1-(2-bromobenzoyl)-4-(4-methoxyphenyl)

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Chamakuri, Srinivas, Sunny Ann Tang, Kevin A. Tran, et al. "A Concise Synthetic Method for Constructing 3-Substituted Piperazine-2-Acetic Acid Esters from 1,2-Diamines." Molecules 27, no. 11 (2022): 3419. http://dx.doi.org/10.3390/molecules27113419.

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We report a short synthetic route for synthesizing 2,3-substituted piperazine acetic acid esters. Optically pure amino acids were efficiently converted into 1,2-diamines that could be utilized to deliver the title 2,3-substituted piperazines in five steps with a high enantiomeric purity. The novel route facilitated, for the first time, the synthesis of 3-phenyl substituted-2-piperazine acetic acid esters that were difficult to achieve using other methods; however, in this case, the products underwent racemization.

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Little, Vanessa Renée, Reid Tingley, and Keith Vaughan. "Triazene derivatives of (1,x)-diazacycloalkanes. Part III. Synthesis and characterization of a series of 1,4-di[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 83, no. 5 (2005): 471–76. http://dx.doi.org/10.1139/v05-064.

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Reaction of a series of diazonium salts with piperazine in a 2:1 molar ratio affords excellent yields of the 1,4-di-[2-aryl-1-diazenyl]piperazines (3), which have been characterized by IR and NMR spectroscopy. Structural characterization is supported by elemental analysis or by mass spectrometry with accurate mass measurement of the molecular ion. The protons of the piperazine ring hydrogens give rise to a sharp singlet at ca. 4 ppm in the NMR spectra, indicating that the conformational equilibrium in the piperazine ring is rapid on the NMR timescale. The four equivalent carbon atoms of the pi

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Sirakanyan, Samvel N., Elmira K. Hakobyan, Athina Geronikaki, et al. "Synthesis and Neurotropic Activity of New 5-Piperazinopyrazolo[3,4-c]-2,7-naphthyridines and Isoxazolo[5,4-c]-2,7-naphthyridines." Pharmaceuticals 18, no. 4 (2025): 597. https://doi.org/10.3390/ph18040597.

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Background/Objectives: Approximately 1% of people worldwide suffer from epilepsy. The development of safer and more effective antiepileptic medications (AEDs) is still urgently needed because all AEDs have some unwanted side effects and roughly 30% of epileptic patients cannot stop having seizures when taking current AEDs. It should be noted that the derivatives of pyrazolo[3,4-b]pyridine are important core structures in many drug substances. The aim of this study is to synthesize new derivatives of piperazino-substituted pyrazolo[3,4-c]-2,7-naphthyridines and 9,11-dimethylpyrimido[1′,2′:1,5]p

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Skov, Joan, Torsten Bryld, Dorthe Lindegaard, et al. "Synthesis and structural characterization of piperazino-modified DNA that favours hybridization towards DNA over RNA." Nucleic Acids Research 39, no. 5 (2010): 1953–65. http://dx.doi.org/10.1093/nar/gkq1123.

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