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Journal articles on the topic 'Piperazine derivatives'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

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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2

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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3

Welz, Anna, Marcin Koba, Piotr Kośliński, and Joanna Siódmiak. "Rapid Targeted Method of Detecting Abused Piperazine Designer Drugs." Journal of Clinical Medicine 10, no. 24 (2021): 5813. http://dx.doi.org/10.3390/jcm10245813.

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Piperazine derivatives belong to the popular psychostimulating compounds from the group of designer drugs. They are an alternative to illegal drugs such as ecstasy and amphetamines. They are being searched by consumers for recreational use due to their stimulating and hallucinogenic effects. Many NPS-related poisonings and deaths have been reported where piperazines have been found. However, a major problem is the potential lack of laboratory confirmation of the involvement of piperazine derivatives in the occurrence of poisoning. Although many methods have been published, piperazine derivativ

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4

Prasad, H. S. Nagendra, A. P. Ananda, Amogh Mukarambi, et al. "Design, synthesis, and anti-bacterial activities of piperazine based phthalimide derivatives against superbug-Methicillin-Resistant Staphylococcus aureus." Current Chemistry Letters 12, no. 1 (2023): 65–78. http://dx.doi.org/10.5267/j.ccl.2022.9.005.

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A series of piperazine-based phthalimide derivatives 5 (a-l) were synthesized and extensively characterized using a variety of spectrum methods, including LC-MS, 1H-NMR, 13C-NMR, and FT-IR. All the derivatives were examined for their physicochemical, pharmacokinetic, bio-activity score, and PASS analysis. The 5e piperazine-based phthalimide derivative demonstrated promising antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) in the in vitro antibacterial studies. In comparison to streptomycin and bacitracin (10 µg/mL), the minimum inhibitory concentration of 5e ag

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5

Němečková, Dana, Eva Havránková, Jan Šimbera, Richard Ševčík, and Pavel Pazdera. "Simplified Procedure for General Synthesis of Monosubstituted Piperazines—From a Batch Reaction Vessel to a Flow (Microwave) Reactor." Molecules 25, no. 9 (2020): 2168. http://dx.doi.org/10.3390/molecules25092168.

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We reported a novel simplified synthetic procedure for the preparation of monosubstituted piperazine derivatives which can now be easily prepared in a one-pot-one-step way from a protonated piperazine with no need of introduction of a protecting group. Reactions, proceeding either at room or higher temperatures in common solvents, involve heterogeneous catalysis by metal ions supported on commercial polymeric resins. A general synthetic scheme was successfully applied to afford a wide range of monosubstituted piperazines. Furthermore, we picked up a set of piperazine derivatives and studied th

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6

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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7

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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8

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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9

Varadaraju, Kavitha Raj, Jajur Ramanna Kumar, Lingappa Mallesha, et al. "Virtual Screening and Biological Evaluation of Piperazine Derivatives as Human Acetylcholinesterase Inhibitors." International Journal of Alzheimer's Disease 2013 (2013): 1–13. http://dx.doi.org/10.1155/2013/653962.

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The piperazine derivatives have been shown to inhibit human acetylcholinesterase. Virtual screening by molecular docking of piperazine derivatives 1-(1,4-benzodioxane-2-carbonyl) piperazine (K), 4-(4-methyl)-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S1), and 4-(4-chloro)-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S3) has been shown to bind at peripheral anionic site and catalytic sites, whereas 4-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S4) and 4-(2,5-dichloro)-benzenesulfonyl-1-(1,4-benzodioxane-2-carbonyl) piperazine (S7) do not bind eith

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10

Wu, Yuet, Silvia Parapini, Ian Williams, et al. "Facile Preparation of N-Glycosylated 10-Piperazinyl Artemisinin Derivatives and Evaluation of Their Antimalarial and Cytotoxic Activities." Molecules 23, no. 7 (2018): 1713. http://dx.doi.org/10.3390/molecules23071713.

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According to the precepts that C-10 amino-artemisinins display optimum biological activities for the artemisinin drug class, and that attachment of a sugar enhances specificity of drug delivery, polarity and solubility so as to attenuate toxicity, we assessed the effects of attaching sugars to N-4 of the dihydroartemisinin (DHA)-piperazine derivative prepared in one step from DHA and piperazine. N-Glycosylated DHA-piperazine derivatives were obtained according to the Kotchetkov reaction by heating the DHA-piperazine with the sugar in a polar solvent. Structure of the D-glucose derivative is se

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11

Li, Wen, Shu-Yi Chen, Wei-Nan Hu, et al. "Design, synthesis, and biological evaluation of quinazoline derivatives containing piperazine moieties as antitumor agents." Journal of Chemical Research 44, no. 9-10 (2020): 536–42. http://dx.doi.org/10.1177/1747519820910384.

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A series of novel quinazoline derivatives containing piperazine analogs are synthesized via substitution reactions with 6,7-disubstituted 4-chloroquinazoline and benzyl piperazine (amido piperazine). Potent antiproliferative activities are observed against A549, HepG2, K562, and PC-3 with N-(3-chlorophenyl)-2-(4-(7-methoxy-6-(3-morpholino-propoxy)quinazoline-4-yl)piperazine-1-yl)acetamidename C9 showing excellent activity. This active derivative was screened for cell migration ability, proliferation effects, and apoptosis against A549 and PC-3 cells, with the result showing biological activity

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12

Al-Masoudi, Najim A., Yaseen A. Al-Soud, Erik De Clercq, and Christophe Pannecouque. "Nitroimidazoles Part 6. Synthesis, Structure and in Vitro anti-HIV Activity of New 5-substituted Piperazinyl-4-nitroimidazole Derivatives." Antiviral Chemistry and Chemotherapy 18, no. 4 (2007): 191–200. http://dx.doi.org/10.1177/095632020701800403.

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2-Amino-1-[4-(1-benzyl-2-ethyl-4-nitro-1 H-imidazol-5-yl)piperazin-1-yl]ethanone [6] was prepared from 1-(1-benzyl-2-ethyl-4-nitro-1 H-imidazol-5-yl) piperazine [3]. A series of new 2-oxoethyl-arylamide [9,10] and 2-oxoethyl-arylsulphonamide [11–14] derivatives were synthesized from [6] with the aim of developing new non-nucleoside reverse transcriptase inhibitors. Alternatively, the amine [17] was synthesized from [3] via the phthalimide derivative [16]. The arylsulphonamide derivatives [18–23] and the arylamide analogues [24–26] were synthesized from [17]. The compounds were evaluated for th

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13

Patel, H. S., H. D. Desai, and H. J. Mistry. "Synthesis and Antimicrobial Activity of Some New Piperazine Derivaties Containing Aryl Sulfonyloxy Group." E-Journal of Chemistry 1, no. 2 (2004): 93–98. http://dx.doi.org/10.1155/2004/732420.

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NovelN-substituted piperazine derivatives containing sulfonyloxy aniline moiety have been prepared. The various 4-sulfonyloxy aniline (SA) derivatives (2a-h) have been prepared by the condensation reaction ofN-Acetyl Sulfanilyl chloride (ASC) and sodium phenates followed by hydrolysis. The SA derivatives are then reacted with chloro acetyl chloride to give corresponding (N-Chloroacetyl) derivatives (3a-h). These derivatives are then reacted withN-phenyl piperazine to yield the corresponding piperazine derivatives (4a-h).

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14

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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15

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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16

Raad, Saad Jihad, Abed Abdul-Reda Nabeel та Mousa Juda Al-Shamari Amer. "Synthesis, characterization and molecular docking of new deriva-tives that contain quіnoxazlіne moities and study antioxidant prop-erties". Pakistan Journal of Analytical & Environmental Chemistry 23, Special Issue (2023): 174–88. https://doi.org/10.5281/zenodo.7702678.

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<strong>   Abstract </strong>     In this study we are prepared some novel derivatives from cetirizine Impurity A by react 1-((4-chlorophenyl)(phenyl) methyl)piperazine with 2-chloro acetyl chloride to prepared 2-chloro-1-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)ethan-1-one (1) from this directive prepared the derivatives (2-6) when react with o-phenylenediamine derivatives to obtain analytically pure quinoxaline derivatives .The reaction was monitored by thin‐layer chromatography (TLC) technique. All new compounds were characterized by melting points, element

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17

Ogurtsov, Vladimir A., and Oleg A. Rakitin. "5,5′-(Piperazine-1,4-diyl)bis(4-chloro-3H-1,2-dithiol-3-one)." Molbank 2022, no. 3 (2022): M1411. http://dx.doi.org/10.3390/m1411.

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Conjugates of 3H-1,2-dithiol-3-ones with various biologically active compounds are intensively investigated. Although many derivatives of this class have been described in the literature, the compounds containing two dithiole cycles have been explored much less. In this communication, it was shown that the reaction of 4,5-dichloro-3H-1,2-dithiol-3-one with piperazine can selectively lead to the mono-product, 4-chloro-5-piperazin-1-yl-3H-1,2-dithiol-3-one and bis-product, 5,5′-(piperazine-1,4-diyl)bis(4-chloro-3H-1,2-dithiol-3-one). The structure of the synthesized compounds was established by

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18

Dileep, Kommula, and M. Murty. "Aqueous, One-Pot, Three-Component Reaction for Efficient Synthesis of 2-[4-(Arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, ‑1H-benzimidazole, or -1,3-benzoxazole Derivatives." Synlett 28, no. 17 (2017): 2295–98. http://dx.doi.org/10.1055/s-0036-1590972.

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A simple and efficient synthetic protocol has been developed involving a one-pot three-component reaction of a 2-chlorobenzazole, piperazine, and an arenesulfonyl chloride under aqueous conditions at room temperature in the absence of a catalyst, ligand, or base. By using this protocol, a variety of 2-[4-(arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, -1H-benzimidazole, and -1,3-benzoxazole derivatives were synthesized in excellent yields.

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19

Loganathan, C. Geethapriya, Karthickeyan Krishnan, S. D. Vachala, Deeparani Urolagin, and J. Vijayakumar. "A Review on 1,2,3 - Triazole & Piperazine Derivatives with Various Biological Activities." Journal of Pharmaceutical Research 22, no. 3 (2023): 113–23. http://dx.doi.org/10.18579/jopcr/v22.3.23.43.

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The largest family of organic molecules in organic chemistry are heterocyclic compounds. A heterocyclic compound is created when an oxygen, nitrogen, sulphur, or atom of a similar element is included in place of a carbon atom. Heterocyclic compounds play a crucial role in daily living. It has a wide scope of uses in agrochemicals and medicinal chemistry. One of a pair of chemical compounds known as triazoles and Piperazine, with the molecular formula C2H3N3 and C5H5N. A fundamental aromatic heterocyclic scaffold is 1,2,3-triazole and piperazine. Because of its structural characteristics, these

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20

Asif, Mohammad. "Piperazine and Pyrazine containing molecules and their diverse pharmacological activities." International Journal of Advances in Scientific Research 1, no. 1 (2015): 05. http://dx.doi.org/10.7439/ijasr.v1i1.1766.

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Efforts were made to synthesize different heterocyclic compounds and their derivatives and were found to posses promising pharmacological compounds. Although piperazine and pyrazine moiety is six membered heterocyclic compounds but is fascinated by scientists because of the diverse biological activities by not only piperazine and pyrazine but its various substituted derivatives as well and having diverse pharmacological activities such antitumor, anticonvulsant, antidepressant, analgesic, antimicrobial, anti?tubercular and anti diabetic, antihistamine, antiinflamatory and other activities. Som

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21

Valenta, Vladimír, Zdeněk Prošek, Jiřina Metyšová, Martin Valchář, Antonín Dlabač, and Miroslav Protiva. "Cataleptic and noncataleptic neuroleptic agents: Synthesis and pharmacology of 4-(2-chloro and 8-chloro substituted 10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine-1-ylalkyl ethers and sulfides." Collection of Czechoslovak Chemical Communications 50, no. 5 (1985): 1070–77. http://dx.doi.org/10.1135/cccc19851070.

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The title compounds Iab-Viab were prepared by substitution reactions of 2,11-dichloro- and 2,10-dichloro-10,11-dihydrodibenzo[b,f]thiepin with 1-(2-methoxyethyl)piperazine, 1-(3-methoxypropyl)piperazine, 1-(2-ethoxyethyl)piperazine, 1-(2-phenoxyethyl)piperazine, 1-(2-methylthioethyl)piperazine and 1-(2-phenylthioethyl)piperazine; they were transformed to hydrochlorides, maleates or methanesulfonates. Compounds of series a (8-chloro derivatives) are neuroleptics, with relatively strong cataleptic, antiapomorphine and central depressant activities (Ia, IIa, IIIa,Va) unless the volume and lipophi

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22

Mamat, Constantin, Marc Pretze, Matthew Gott, and Martin Köckerling. "Synthesis, dynamic NMR characterization and XRD studies of novel N,N’-substituted piperazines for bioorthogonal labeling." Beilstein Journal of Organic Chemistry 12 (November 21, 2016): 2478–89. http://dx.doi.org/10.3762/bjoc.12.242.

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Novel, functionalized piperazine derivatives were successfully synthesized and fully characterized by 1H/13C/19F NMR, MS, elemental analysis and lipophilicity. All piperazine compounds occur as conformers resulting from the partial amide double bond. Furthermore, a second conformational shape was observed for all nitro derivatives due to the limited change of the piperazine chair conformation. Therefore, two coalescence points were determined and their resulting activation energy barriers were calculated using 1H NMR. To support this result, single crystals of 1-(4-nitrobenzoyl)piperazine (3a,

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23

Patel, Nalini, Vaishali Karkhanis, and Pinkal Patel. "Synthesis and Biological Evaluation of Some Piperazine Derivatives as Anti-Inflammatory Agents." Journal of Drug Delivery and Therapeutics 9, no. 4-s (2019): 353–58. http://dx.doi.org/10.22270/jddt.v9i4-s.3327.

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Some 1-((4-methylpiperazin-1yl)methyl)-1H-benzo[d]imidazole & 1-((4-phenylpiperazin-1yl)methyl)-1H-benzo[d]imidazole derivatives were synthesized through reaction of 1-substituted piperazines with different benzimidazole derivatives in methanol yielded the corresponding mannich bases (42-a to 42-i). All the synthesized compounds were elucidated by IR, 1H NMR and MASS spectroscopy. They were tested for anti-inflammatory activity using in-vivo (Carrageenan- induced rat paw edema model) method at a dose of 50mg/kg. result showed that compounds 42-c, 42-d and 42-h were found to be most potent

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24

Kracht, Daniel, Susumu Saito, and Bernhard Wünsch. "Synthesis of 1,4-Diazabicyclo[3.3.1]nonan-6-ones." Australian Journal of Chemistry 62, no. 12 (2009): 1684. http://dx.doi.org/10.1071/ch09206.

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1,4-Diazabicyclo[3.3.1]nonanes (aza-morphans) represent conformationally constrained piperazine derivatives. Herein, we report a six-step synthesis of the benzyl and allyl substituted bicyclic ketones 3a and 3b, which represent interesting building blocks for the synthesis of conformationally restricted receptor ligands. The key steps of the synthesis are the regioselective addition of ethyl acrylate to the piperazine 8, the sodium hexamethyldisilazide-induced Dieckmann cyclization of the diesters 10, and the decarboxylation of the enol esters 11 with dilute HCl. The complete sequence is only

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Krishnaswamy, G., Nivedita R. Desai, Naika H. Raja, S. Sreenivasa, and Kumar D. B. Aruna. "Synthesis of novel 5-(4-N-Alkyl-piperazin-1-yl)-1-benzofuran-2-yl)-3-substituted phenyl propenone derivatives as antibacterial agents: In vitro and In silico studies." Research Journal of Chemistry and Environment 27, no. 1 (2022): 78–85. http://dx.doi.org/10.25303/2701rjce078085.

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The present study aimed at the synthesis and in vitro as well as in silico evaluation of novel 5-(4-N-alkyl-piperazin-1-yl)-1-benzofuran-2-yl)-3-substituted phenyl propenone [3a-f] derivatives as antibacterial agents. The structures of newly synthesized compounds were characterized by spectroscopic techniques such as FT-IR, 1HNMR and mass spectrometry. Finally, the newly synthesized derivatives were screened for their in vitro antibacterial activities and exhibited weak to moderate activity. N-alkyl piperazine benzofuran derivatives exhibited good activity while their corresponding chalcone de

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Qasid, Muhammad, Ayaz Ahmad, and Talal Ahmed. "REVIEW ANALYSIS ON SYNTHESIS, ENZYME INHIBITION AND HEMOLYTIC STUDY OF NOVEL ACETAMIDE DERIVATIVES." Journal of Technology & Innovation 4, no. 1 (2024): 01–10. https://doi.org/10.26480/jtin.01.2024.01.10.

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The synthesis of 2- (2,4-dichloro-6-{[4-(2-furoyl)-1-piperazine]sulfonyl}phenoxy)-N-(aryl) acetamides was carried out under the controlled conditions as mentioned in the scheme. In the first step, the nucleophile is formed by reacting the calculated amount of N-(2-furoyl) piperazine (1) with 3,5-dichloro-2-hydroxybenzenesulfonylchloride (2) in the presence of an aqueous solution of sodium carbonate and stirred for three hours at room temperature to produce{4-[(3,5-dichloro-2-hydroxyphenyl)sulfonyl]-1-piperazinyl}(2-furoyl)methanone (3). In the parallel set of reactions, electrophile was prepar

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27

Wenceslau, João P. S., Dávila F. de Souza, Maria C. F. de Oliveira, et al. "Novel Lapachol Derivatives and Their Antioxidant Activity." Natural Product Communications 1, no. 8 (2006): 1934578X0600100. http://dx.doi.org/10.1177/1934578x0600100812.

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A convenient synthesis of the new enamine derivatives 2-diethylamino-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (2), 2-ethylamino-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (3), 2-diethanolamino-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (4), and 2-(1-piperazinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (5) was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphtalenedione (lapachol, 1) and diethylamine, ethylamine, diethanolamine and piperazine, respectively. All products were fully characterized by IR, 1H and 13C NMR spectroscopy. Results revealed no antioxidant behavio

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28

Kaya, Betül, Yusuf Özkay, Halide Edip Temel, and Zafer Asım Kaplancıklı. "Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives." Journal of Chemistry 2016 (2016): 1–7. http://dx.doi.org/10.1155/2016/5878410.

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Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR,1H-NMR,13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds3a–kagainst AChE and BuChE was measured and evaluated using a modification of Ellman’s spectrophotomet

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29

Babu, Donka Suresh, Doddaga Srinivasulu, Valaparla Bala Yesu, et al. "SYNTHESIS AND EVALUATION OF SOME NEW SUBSTITUTED PIPERAZINYL-ARYL AMIDE, ACETAMIDE, AND SULFONAMIDE DERIVATIVES OF ROSUVASTATIN INTERMEDIATE AND THEIR ANTI-MICROBIAL ACTIVITY." RASAYAN Journal of Chemistry 16, no. 01 (2023): 527–35. http://dx.doi.org/10.31788/rjc.2023.1618008.

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In pursuit of a biodynamically potent molecule, we have attempted to synthesize derivatives of piperazine by incorporating them into the Rosuvastatin intermediate. The reason behind this is that heterocyclic compounds with nitrogen atoms in their ring structure, such as pyrimidine, have great potential as drug design scaffolds. By doping piperazine into the Rosuvastatin intermediate, a series of new derivatives made up of aryl-amides, acetamides, and sulfonamides were produced. These derivatives were then assessed for their antimicrobial activity, with a few showing promising results.

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Patel, Priteshkumar Rajeshbhai, Joshi Hirak, Shah Ujash, Patel Bhagirath, and Bapna Mayank. "Novel Piperazine Derivatives as Anti Microbial Agents: A Comprehensive Review." Asian Pacific Journal of Health Sciences 9, no. 2 (2022): 36–39. http://dx.doi.org/10.21276/apjhs.2022.9.2.09.

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Over the past decade, there has been an increased development of resistance in organisms that are typical pathogenic in humans. This increased resistance has limited the selection of antimicrobials that may be used to treat specific organisms. Therefore, there is demanding to develop novel classes of drugs, with fewer side effects, and shorter lengths of treatment are key in continuing the fight against infectious disease. In the search of newer antimicrobial agents, various heterocyclic compounds have been examined and out of them, Piperazine derivatives have exhibited diverse biological acti

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Ostrowska, Kinga, Anna Leśniak, Weronika Gryczka, Łukasz Dobrzycki, Magdalena Bujalska-Zadrożny, and Bartosz Trzaskowski. "New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT1A Receptor Agents." International Journal of Molecular Sciences 24, no. 3 (2023): 2779. http://dx.doi.org/10.3390/ijms24032779.

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A series of 15 new derivatives of 6-acetyl-7-hydroxy-4-methylcoumarin containing a piperazine group were designed with the help of computational methods and were synthesized to study their affinity for the serotonin 5-HT1A and 5-HT2A receptors. Among them, 6-acetyl-7-{4-[4-(3-bromophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (4) and 6-acetyl-7-{4-[4-(2-chlorophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (7) exhibited excellent activity for 5-HT1A receptors with Ki values 0.78 (0.4–1.4) nM and 0.57 (0.2–1.3) nM, respectively, comparable to the Ki values of 8-OH-DPAT (0.25 (0.097–0.

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Andric, Deana, Gordana Tovilovic, Goran Roglic, et al. "Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives." Journal of the Serbian Chemical Society 72, no. 5 (2007): 429–35. http://dx.doi.org/10.2298/jsc0705429a.

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Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, expressed higher affinities for all receptor classes than clozapi

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Osmaniye, Derya, Ramazan Alaşan, Begüm Nurpelin Sağlık, Serkan Levent, Yusuf Özkay, and Zafer Asım Kaplancıklı. "Novel thiazolyl-hydrazone derivatives including piperazine ring: synthesis, in vitro evaluation, and molecular docking as selective MAO-A inhibitor." Zeitschrift für Naturforschung C 77, no. 3-4 (2021): 167–75. http://dx.doi.org/10.1515/znc-2021-0223.

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Abstract MAO-A inhibitors are used in the treatment of depression. There are many studies showing that the thiazolyl-hydrazone structure is a pharmacophore structure for the MAO enzyme. In previous studies by our team, activity studies were carried out with thiazolyl-hydrazone derivatives containing pyrrolidine, morpholine, and piperazine. All of them were displayed MAO-A selective inhibition profile. Additionally, derivatives containing piperazine ring were most active. For this purpose, thiazolyl-hydrazone derivatives containing piperazine were synthesized, but this time an active group, for

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Badran, TW, and CJ Easton. "Monosubstitution of Symmetrical Piperazine-2,5-dione Derivatives." Australian Journal of Chemistry 43, no. 8 (1990): 1455. http://dx.doi.org/10.1071/ch9901455.

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Welz, Anna, and Marcin Koba. "Piperazine derivatives as dangerous abused compounds." Acta Pharmaceutica 70, no. 4 (2020): 423–41. http://dx.doi.org/10.2478/acph-2020-0035.

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AbstractPiperazine derivatives are a group of compounds with a psychostimulant effect. They are an alternative to illegal drugs. They are being searched for recreational use due to their psychoactive and hallucinogenic effects. The high popularity of these compounds can be noticed all over the world due to easy purchase, lack of legal regulations and incorrect assessment of the safety of use. The recreational use of piperazine derivatives can often result in chronic and acute health problems and additionally with unpredictable remote effects. It is also common to take mixtures of psychoactive

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Sonkamble, Sneh D., Dinesh D. Rishipathak, Laxman A. Kawale, and Vandana S. Nade. "DESIGN, SYNTHESIS AND EVALUATION OF CNS DEPRESSANT ACTIVITY OF 2-(SUBSTITUTED ARYL)-PIPERAZINE-3-PHENYL-4(3H)-QUINAZOLINONE." International Journal of Pharmaceutical Sciences and Drug Research 15, no. 02 (2023): 209–13. http://dx.doi.org/10.25004/ijpsdr.2023.150213.

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Anxiety is characterized by excessive fear that persists and interferes with a person's daily activities. In this study, a new class of 16 derivatives of 2-(Substituted Aryl)-piperazine-3-phenyl-4(3H)-quinazolinones were synthesized, and all of the derivatives were tested for their ability to reduce anxiety using the holeboard test and the elevated plus maize test, administered intraperitoneally to mice at doses of 10 mg/kg body weight. Test compounds 3-phenyl-2-(4-(3-methylphenyl) piperazin-1-yl)quinazolin-4(3H)-one (SD-05), 2-(4-(2-fluorophenyl) piperazin-1-yl)-3-phenylquinazolin-4(3H)-one (

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Thirunavukarasu, Jayaprakash, and Abdul Rahim Shajahan. "Antidiabetic and Anti-inflammatory Properties of N-Phenyl Piperazine Derivatives through In Vitro Evaluations and Molecular Docking Studies." Biomedical and Pharmacology Journal 18, no. 2 (2025): 1517–29. https://doi.org/10.13005/bpj/3188.

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N-phenyl Piperazine derivatives have increasingly been recognized for their profound medicinal properties. This study embarks on the synthesis and study of such derivatives, specifically focusing on their in vitro α-amylase inhibitory and anti-inflammatory potential. Employing in silico molecular docking strategies, we assessed the interactions of these derivatives with the α-amylase enzyme (1HNY.pdb). Compounds P6, P7, and P22 emerged with commendable docking scores as -8.44, -8.37, and -8.49 kcal/mol, prompting their synthesis and assessment of in vitro α-amylase activity assessment. Among t

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Moshafi, Hassan, Azadeh Yahya-Meymandi, Esmaeil Sadat-Ebrahimi, et al. "Synthesis and biological activity of 5-nitrofuran-containing (1,3,4-thiadiazol-2-yl)piperazine moieties as a new type of anti-Helicobacter pylori heterocycles." Journal of the Serbian Chemical Society 76, no. 2 (2011): 201–10. http://dx.doi.org/10.2298/jsc100324013m.

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In order to find new and potent drug candidates for the treatment of Helicobacter pylori infections? in this study attention was focused on the synthesis and anti-H. pylori activity of a series of 5-(5-nitrofuran-2- yl)-1,3,4-thiadiazoles containing piperazinyl functionality at the C-2 position of the 1,3,4-thiadiazole ring. The synthesis of 1-[5-(5-nitrofuran- 2-yl)-1,3,4-thiadiazol-2-yl]piperazine derivatives (3a-h) and pyrrolidine derivative 3i was achieved with a versatile and efficient synthetic route via 2-chloro-5-(5-nitrofuran-2-yl)-1,3,4-thiadiazole. The inhibitory activity of the new

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Mizuki, Y., I. Fujiwara, T. Yamaguchi, and Y. Sekine. "Structure-related inhibitory effect of antimicrobial enoxacin and derivatives on theophylline metabolism by rat liver microsomes." Antimicrobial Agents and Chemotherapy 40, no. 8 (1996): 1875–80. http://dx.doi.org/10.1128/aac.40.8.1875.

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Enoxacin, an antimicrobial fluoroquinolone with a 7-piperazinyl-1, 8-naphthyridine skeleton, is a potent inhibitor of cytochrome P-450-mediated theophylline metabolism. The present study was designed to clarify, using seven enoxacin derivatives, the molecular characteristics of the fluoroquinolone responsible for the inhibition. Three derivatives with methyl-substituted 7-piperazine rings inhibited rat liver microsomal theophylline metabolism to 1,3-dimethyluric acid to an extent similar to that of enoxacin (50% inhibitory concentrations [IC50s] = 0.39 to 0.48 mM). 7-Piperazinyl-quinoline deri

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Vejdělek, Zdeněk, and Miroslav Protiva. "1-(4-Cyclopentylphenyl)piperazine and its 4-substituted derivatives; Synthesis and biological screening." Collection of Czechoslovak Chemical Communications 52, no. 7 (1987): 1834–40. http://dx.doi.org/10.1135/cccc19871834.

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Heating the hydrochlorides of 4-cyclopentylaniline and diethanolamine to 250 °C gave 1-(4-cyclopentylphenyl)piperazine (I). Acylation of I with ethyl formate and the corresponding acyl chlorides gave the amides II, VI, and VII which were reduced with lithium aluminium hydride to the piperazines III, VIII, and IX. Treatment of I with benzyl chloride and with 4-chloro-1-(4-fluorophenyl)butan-1-one under different conditions led to compounds IX and XI. Addition reaction of I to 1,2-epoxybutane resulted in the amino alcohol V. The products showed marginal tranquillizing activity (especially compou

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Al-Soud, Yaseen A., Ala’a H. Al-Ahmad, Luay Abu-Qatouseh, et al. "Nitroimidazoles Part 9. Synthesis, molecular docking, and anticancer evaluations of piperazine-tagged imidazole derivatives." Zeitschrift für Naturforschung B 76, no. 5 (2021): 293–302. http://dx.doi.org/10.1515/znb-2020-0200.

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Abstract New piperazine-tagged imidazole derivatives were synthesized via reaction of 1-alkyl/aryl-5-bromo-2-alkyl-4-nitro-1H-imidazoles 1–3 with piperazine nucleophiles. Nine selected compounds were assessed for their antiproliferative inhibition potency against five human cancer cell lines (MCF-7, PC3, Du145, HepG2 and Dermal/Fibroblast). Compounds 7 and 10 are the most potent anticancer agents on HepG2 cell line with IC50 values of (5.6 ± 0.5 µm) and (29.6 ± 7.6 µm) respectively, and on MCF-7 with IC50 values of (32.1 ± 5.6 µm) and (46.2 ± 8.2 µm) respectively. The molecular docking of comp

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SARI, Sait, and Mehmet YILMAZ. "Synthesis and characterization of piperazine-substituted dihydrofuran derivatives viaMn(OAc)3 mediated radical cyclizations." TURKISH JOURNAL OF CHEMISTRY 44, no. 5 (2020): 1303–13. http://dx.doi.org/10.3906/kim-2003-23.

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The aim of this study is to synthesize novel piperazine-containing dihydrofuran compounds (3a-n)from radical additions and cyclizations of diacyl and alkyl-acyl piperazine derivatives (1a-h) with 1,3-dicarbonyl compounds (2a-c) mediated by Mn(OAc)3 for the first time. From the reactions of 1a-c with dimedone (2a);1a, 1c, and 1d with acetylacetone (2b); and 1a with ethylacetoacetate(2c) ,the dihydrofuran-piperazine compounds 3a-c, 3d-f, and 3g were obtained in medium to high yields (31%–81%), respectively. In addition, dihydrofuran-piperazine compounds 3h-j and 3k-n were prepared at low to medi

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Zsoldos, Bernadett, Nóra Nagy, Viktória Donkó-Tóth, et al. "Novel Piperazine Derivatives of Vindoline as Anticancer Agents." International Journal of Molecular Sciences 25, no. 14 (2024): 7929. http://dx.doi.org/10.3390/ijms25147929.

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A series of novel vindoline–piperazine conjugates were synthesized by coupling 6 N-substituted piperazine pharmacophores at positions 10 and 17 of Vinca alkaloid monomer vindoline through different types of linkers. The in vitro antiproliferative activity of the 17 new conjugates was investigated on 60 human tumor cell lines (NCI60). Nine compounds presented significant antiproliferative effects. The most potent derivatives showed low micromolar growth inhibition (GI50) values against most of the cell lines. Among them, conjugates containing [4-(trifluoromethyl)benzyl]piperazine (23) and 1-bis

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Patel, Divyesh, Rahul Patel, Premlata Kumari, and Navin B. Patel. "Synthesis of s-Triazine-Based Thiazolidinones as Antimicrobial Agents." Zeitschrift für Naturforschung C 67, no. 3-4 (2012): 108–22. http://dx.doi.org/10.1515/znc-2012-3-402.

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5A novel series of thiazolidinone derivatives, namely 4-{4-dimethylamino-6-[4-oxo- 2-phenyl-5-(4-pyridin-2-yl-piperazin-1-ylmethyl)-thiazolidin-3-yl]-[1,3,5]-triazin-2-yloxy}- 1-methyl-1H-quinolin-2-ones, have been synthesized from the key intermediate 4-(4-amino- 6-dimethylamino-[1,3,5]-triazin-2-yloxy)-1-methyl-1H-quinolin-2-one (). Compound 5 was condensed with various aldehydes to give Schiff base derivatives, which after cyclization gave thiazolidinones that were linked with 1-pyridin-2-yl-piperazine to obtain the target compounds. The newly synthesized compounds were evaluated for their

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Szczepanska, Katarzyna, Kamil Kuder, and Katarzyna Kiec-Kononowicz. "Histamine H3 Receptor Ligands in the Group of (Homo)piperazine Derivatives." Current Medicinal Chemistry 25, no. 14 (2018): 1609–26. http://dx.doi.org/10.2174/0929867325666171123203550.

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Since its discovery in 1983, followed by gene cloning in 1999, the histamine H3 receptor served as an outstanding target for drug discovery. The wide spectrum of possible therapeutic implications makes H3R's one of the most researched areas in the vast GPCR ligands field - started from imidazole containing ligands, through various successful imidazole replacements, with recent introduction of Wakix® to pharmaceutical market. One such replacement is piperazine moiety, a significant versatile scaffold in rational drug design for most of the GPCR ligands. Therefore, herein, we review ligands buil

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Devender, Pathak, Lata Pandey Suman, and Kumar Nitin. "Synthesis, characterization and in vivo anthelmintic activity of some newer piperazine derivatives." Journal of Indian Chemical Society Vol. 89, May 2012 (2012): 683–88. https://doi.org/10.5281/zenodo.5763407.

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Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, N.H. #2 Delhi-Mathura Bye-pass, P.O. Chhatikara, Mathura-281 001, Uttar Pradesh, India <em>E-mail</em> : dev_15@rediffmail.com <em>Manuscript received 24 May 2011, revised 30 August 2011, accepted 07 September 2011</em> Substituted primary aromatic amines on diazotization gives diazonium salt which on reaction with various piperazine derivatives get converted into diazotized product 3a-e, 4a-e and Sb-c. The structures of the newly synthesized piperazine derivatives were accomplished through IR, <sup>1</sup>H NMR and m

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Melent’ev, A. B., and S. S. Kataev. "Metabolism of designer drugs. Piperazine derivatives." Sudebno-meditsinskaya ekspertiza 58, no. 4 (2015): 49. http://dx.doi.org/10.17116/sudmed201558349-55.

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Pinter, A., G. B. Spiegelhalder, G. Török, et al. "Genotoxicity of N-nitroso-piperazine derivatives." Toxicology Letters 95 (July 1998): 44–45. http://dx.doi.org/10.1016/s0378-4274(98)80175-6.

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Pascal, Jean-Claude, Henri Pinhas, Francette Laure, Danièle Dumez, and Alain Poizot. "New antiarrhythmic agents. Piperazine guanidine derivatives." European Journal of Medicinal Chemistry 25, no. 1 (1990): 81–85. http://dx.doi.org/10.1016/0223-5234(90)90169-4.

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Lattermann, G., S. Schmidt, and B. Gallot. "Liquid crystalline piperazine and triazacyclononane derivatives." Journal of the Chemical Society, Chemical Communications, no. 15 (1992): 1091. http://dx.doi.org/10.1039/c39920001091.

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