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Journal articles on the topic 'Substituted Piperazines'

Author: Grafiati

Published: 5 June 2025

Last updated: 1 August 2025

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1

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

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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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2

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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3

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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4

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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5

Wierschem, Frank, and Karola Rück-Braun. "Introduction of Substituents on the 2-Oxo-piperazine Skeleton by [3+2] Cycloaddition and Subsequent Transformation." Zeitschrift für Naturforschung B 61, no. 4 (2006): 431–36. http://dx.doi.org/10.1515/znb-2006-0410.

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The 3,4-substituted 2-oxo-piperazines 5 - 9 are obtained by [3+2] cycloaddition from nitrone 1 and a variety of alkenes. Subsequent functionalization of the bicyclic adducts involves reductive N-O bond cleavage. A route towards libraries of immobilized 1,3-aminoalcohols with a 3,4-substituted 2-oxo-piperazine scaffold is briefly discussed for adducts derived from N-substituted maleic imides

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6

Abdel-Jalil, Raid J., Muhammad Saeed, Peter Heeg, and Wolfgang Voelter. "Synthesis and Properties of Selected 4-Substituted Anhydro Sugars." Zeitschrift für Naturforschung B 55, no. 7 (2000): 661–66. http://dx.doi.org/10.1515/znb-2000-0714.

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A new class of 4-deoxy-4-([4-substituted-1-piperazinyl], [4-morpholinyl] and [4-(perhydrol, 4-thiazin-4-yl)])-2,3-anhydrolyxopyranosides (3a-g and 6a-g) were synthesized from epoxy triflate moities 2 and 5 and 4-substituted piperazines, morpholines and perhydro-1,4- thiazines, respectively, to test their antibacterial activity. The characterized series of new compounds was tested in vitro against E. coli ATCC11229, S. aureus ATCC6538 and C. albicans SATCC10231.

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7

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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8

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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9

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

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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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10

Clifford, Sarah E., Vanny Tiwow, Aleasia Gendron, et al. "Complexation of Constrained Ligands Piperazine, N-substituted Piperazines, and Thiomorpholine." Australian Journal of Chemistry 62, no. 10 (2009): 1196. http://dx.doi.org/10.1071/ch09313.

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Complexation of the symmetric cyclic diamine piperazine (1,4-diazacyclohexane) has been examined in dry dimethyl formamide by spectrophotometric titrations (with Cu2+, Ni2+) to define formation constants, and by stopped-flow kinetics to define the complexation rates and reaction pathway. Initial formation of a rarely observed η1-piperazine intermediate occurs in a rapid second-order reactions. This intermediate then undergoes two competing reactions: formation of (chelated) η2-piperazine (ML) or the formation of (bridging) μ-piperazine (in M2L and M2L3, speciation depending on relative concent

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11

Möhrle, Hans, and Katja Azodi. "Reaktionen Von Acetylencarbonsäureestern Mit Piperazinderivaten." Zeitschrift für Naturforschung B 61, no. 8 (2006): 1021–34. http://dx.doi.org/10.1515/znb-2006-0815.

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Hg(II)-EDTA-dehydrogenation of benzylpiperazine (5) in 50% ethanol with addition of diethyl acetylenedicarboxylate (2) to a minor extent gives rise to (piperazine-1,4-diyl)-bis(maleate) (9), which is inert to Hg(II)-EDTA and results in quantitative yield when Hg(II)-EDTA is omitted. 4- Benzylpiperazin-1-yl)-monomaleate (8) reacts with 2 in various solvents by addition of water with dealkylation and formation of 9. CH-acidic compounds may also be used as proton donors. Analogous reactions, although with minor yields, occur with the propiolates 11 and 12. 1-Substituted piperazines with benzyl, m

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12

Sati, Nitin, Sushil Kumar, and Sushil Sati. "Synthesis and Pharmacological Evaluation of 7-{2-[4-(Substituted phenyl)-piperazin-1-yl]-2-Oxo-Ethoxy}-4-Methyl-Chromen-2-Ones as Serotonin 5-HT2 Receptors Antagonist." International Journal of Drug Design and Discovery 2, no. 1 (2024): 419–24. https://doi.org/10.37285/ijddd.2.1.9.

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Substitutedphenyl piperazines were treated with chloroacetylchloride to give respective 2-chloro-1-[4-(substitutedphenyl)-piperazin-1-yl]-ethanones which were subsequently coupled to 7-hydroxy-4-methyl-chromen-2-one to afford the target compounds 7-{2-[4-(substituted phenyl)-piperazin-1-yl]-2-oxo-ethoxy}-4-methyl-chromen-2-ones. The novel compounds were evaluated in-vivo for antagonism at serotonin 5-HT2 receptor. Some of the compounds synthesized showed high antagonistic activity for the target receptor. The binding affinity to these receptors depended greatly on the nature and position of su

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13

Chamakuri, Srinivas, Manuj M. Shah, David C. H. Yang, Conrad Santini, and Damian W. Young. "Practical and scalable synthesis of orthogonally protected-2-substituted chiral piperazines." Organic & Biomolecular Chemistry 18, no. 43 (2020): 8844–49. http://dx.doi.org/10.1039/d0ob01713b.

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14

Šilhánková, Alexandra, Karel Šindelář, Karel Dobrovský, Ivan Krejčí, Jarmila Hodková, and Zdeněk Polívka. "Synthesis of New L-Proline Amides with Anticonvulsive Effect." Collection of Czechoslovak Chemical Communications 61, no. 7 (1996): 1085–92. http://dx.doi.org/10.1135/cccc19961085.

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Series of heterocyclic L-proline amides were prepared from BOC-L-proline and heterocyclic amines (mostly substituted piperazines and morpholines) via active ester with hydroxysuccinimide. 4-(4-Fluorobenzoyl)piperidine afforded L-proline 4-(4-(4-(4-fluorobenzoyl)piperidin-1-yl)benzoyl)piperidine (7b) simultaneously with expected L-proline 4-(4-fluorobenzoyl)piperidide (7a). D-Proline N-(3-(4-(3-chlorophenyl)piperazin-1-yl)propyl)amide (2) was prepared starting from D-proline. The amides were tested by methods of biochemical and behavioural pharmacology.

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15

Dolan, Sean B., Ritu A. Shetty, Michael J. Forster, and Michael B. Gatch. "Impure but not inactive: Behavioral pharmacology of dibenzylpiperazine, a common by-product of benzylpiperazine synthesis." Journal of Psychopharmacology 32, no. 7 (2018): 802–10. http://dx.doi.org/10.1177/0269881118780613.

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Background: Substituted piperazines comprise a substantial proportion of the novel psychoactive substance market. Among the most widely abused piperazine compounds are meta-chlorophenylpiperazine (mCPP), tri-fluoromethylphenylpiperazine (TFMPP), and, especially, benzylpiperazine (BZP), which are commonly incorporated, either alone or in combination, in illicit “party pills” or “ecstasy” formulations. Illicit synthesis of BZP often results in production of an impure by-product dibenzylpiperazine (DBZP), which frequently appears alongside BZP in these formulations; however, despite its ubiquity,

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16

Kallel, E. Adam, Colin Vangel, and Daniel Elbaum. "Conformational analysis of 2-substituted piperazines." Bioorganic & Medicinal Chemistry Letters 26, no. 13 (2016): 3010–13. http://dx.doi.org/10.1016/j.bmcl.2016.05.022.

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17

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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18

Raghavendra, N. M., P. P. Thampi, and P. M. Gurubasavarajaswamy. "Synthesis and Antimicrobial Activity of Some Novel Substituted Piperazinyl-quinazolin-3(4H)-ones." E-Journal of Chemistry 5, no. 1 (2008): 23–33. http://dx.doi.org/10.1155/2008/410157.

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Several substituted-quinazolin-3(4H)-ones were synthesized by condensation of 2-chloro-N-(4-oxo-substituted-quinazolin-3(4H)-yl)-acetamides with various substituted piperazines through single step reaction. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolin-4-one derivatives were investigated for their antibacterial and antifungal activities.

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19

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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20

Narczyk, Aleksandra, та Sebastian Stecko. "An entry to non-racemic β-tertiary-β-amino alcohols, building blocks for the synthesis of aziridine, piperazine, and morpholine scaffolds". Organic & Biomolecular Chemistry 18, № 30 (2020): 5972–81. http://dx.doi.org/10.1039/d0ob01315c.

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The synthesis of α-dialkyl-substituted non-racemic allyl alcohols and their transformation into enantiomerically enriched 1,1-dialkylated 1,2-aminoalcohols, aziridines, morpholines and piperazines is reported.

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21

Jida, Mouhamad, та Steven Ballet. "Efficient one-pot synthesis of enantiomerically pure N-protected-α-substituted piperazines from readily available α-amino acids". New Journal of Chemistry 42, № 3 (2018): 1595–99. http://dx.doi.org/10.1039/c7nj04039c.

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A new pathway towards enantiomerically pure 3-substituted piperazines, bearing a benzyl protecting group, has been developed in good overall yields (83–92%), starting from commercially available N-protected amino acids.

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22

Filipova, Alzbeta, Jan Marek, Radim Havelek, et al. "Substituted Piperazines as Novel Potential Radioprotective Agents." Molecules 25, no. 3 (2020): 532. http://dx.doi.org/10.3390/molecules25030532.

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The increasing risk of radiation exposure underlines the need for novel radioprotective agents. Hence, a series of novel 1-(2-hydroxyethyl)piperazine derivatives were designed and synthesized. Some of the compounds protected human cells against radiation-induced apoptosis and exhibited low cytotoxicity. Compared to the previous series of piperazine derivatives, compound 8 exhibited a radioprotective effect on cell survival in vitro and low toxicity in vivo. It also enhanced the survival of mice 30 days after whole-body irradiation (although this increase was not statistically significant). Tak

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23

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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24

JYOTI, JAIN, and K. SRIVASTAVA SANTOSH. "Synthesis of Novel N-Substituted Phenothiazines and Piperazines as Potential Biologically Active Agents." Journal of Indian Chemical Society Vol. 71, Nov 1994 (1994): 691–92. https://doi.org/10.5281/zenodo.5897641.

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Department of Chemistry, Dr. H. S. Gour University, Sagar-470 003 Manuscript received 23 April 1993, revised 30 August 1993, accepted 17 September 1993 Synthesis of Novel <em>N</em>-Substituted Phenothiazines and Piperazines as Potential Biologically Active Agents

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25

SUNITA, CHAURASIA, та D. SRIVASTAVA SAVITRI. "Synthesis and Antimicrobial Activity of N-[α-(Phenoxy/Substituted-phenoxy)acetyl/propionyl]piperazines/morpholines". Journal of Indian Chemical Society Vol. 69, Jan 1992 (1992): 45–46. https://doi.org/10.5281/zenodo.6132984.

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Department of Chemistry, Dr. Harisingh Gour Vishwavidyalaya, Sagar-470 003 <em>Manuscript received 27 May 1991, revised 21 November 1991, accepted 6 January 1992</em> Synthesis and Antimicrobial Activity of <em>N</em>-[α-(Phenoxy/Substituted-phenoxy)acetyl/propionyl]piperazines/morpholines.

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26

Santes, Víctor, Elizabeth Gómez, Rosa Santillan, and Norberto Farfán. "Facile Deuteration of Chiral N,N′-Substituted Piperazines." Synthesis 2001, no. 02 (2001): 0235–38. http://dx.doi.org/10.1055/s-2001-10810.

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27

Abdel-Jalil, Raid J., Raed A. Al-Qawasmeh, Yousef Al-Abed, and Wolfgang Voelter. "A stereospecific synthesis of tetra-substituted chiral piperazines." Tetrahedron Letters 39, no. 42 (1998): 7703–4. http://dx.doi.org/10.1016/s0040-4039(98)01677-3.

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28

Troshina, Olesya A., Pavel A. Troshin, Alexander S. Peregudov, Elena M. Balabaeva, Vyacheslav I. Kozlovski, and Rimma N. Lyubovskaya. "Reactions of chlorofullerene C60Cl6 with N-substituted piperazines." Tetrahedron 62, no. 43 (2006): 10147–51. http://dx.doi.org/10.1016/j.tet.2006.08.033.

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29

Zhai, Huimin, Andrey Borzenko, Ying Yin Lau, Shin Hye Ahn, and Laurel L. Schafer. "Catalytic Asymmetric Synthesis of Substituted Morpholines and Piperazines." Angewandte Chemie 124, no. 49 (2012): 12385–89. http://dx.doi.org/10.1002/ange.201206826.

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30

Brockunier, Linda L., Jiafang He, Lawrence F. Colwell, et al. "Substituted piperazines as novel dipeptidyl peptidase IV inhibitors." Bioorganic & Medicinal Chemistry Letters 14, no. 18 (2004): 4763–66. http://dx.doi.org/10.1016/j.bmcl.2004.06.065.

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31

Veselkina, O. S., I. L. Solovtsova, N. N. Petrishchev, et al. "Influence of N,N′-Substituted Piperazines on Cytolysis." Pharmaceutical Chemistry Journal 49, no. 11 (2016): 743–48. http://dx.doi.org/10.1007/s11094-016-1363-8.

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32

Pukhov, S. A., S. V. Afanas’eva, L. V. Anikina, V. I. Kozlovskii, M. E. Neganova, and S. G. Klochkov. "Cytotoxicity of Natural Alantolactones Conjugated to Substituted Piperazines." Chemistry of Natural Compounds 55, no. 1 (2019): 41–46. http://dx.doi.org/10.1007/s10600-019-02611-z.

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33

Zhai, Huimin, Andrey Borzenko, Ying Yin Lau, Shin Hye Ahn, and Laurel L. Schafer. "Catalytic Asymmetric Synthesis of Substituted Morpholines and Piperazines." Angewandte Chemie International Edition 51, no. 49 (2012): 12219–23. http://dx.doi.org/10.1002/anie.201206826.

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34

Al-Wahaibi, Lamya H., Ahmed A. B. Mohamed, Samar S. Tawfik, Hanan M. Hassan, and Ali A. El-Emam. "1,3,4-Oxadiazole N-Mannich Bases: Synthesis, Antimicrobial, and Anti-Proliferative Activities." Molecules 26, no. 8 (2021): 2110. http://dx.doi.org/10.3390/molecules26082110.

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The reaction of 5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione 3 with formaldehyde solution and primary aromatic amines or 1-substituted piperazines, in ethanol at room temperature yielded the corresponding N-Mannich bases 3-arylaminomethyl-5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones 4a–l or 3-[(4-substituted piperazin-1-yl)methyl]-5-(3,4-dimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thiones 5a–d, respectively. The in vitro inhibitory activity of compounds 4a–l and 5a–d was assessed against pathogenic Gram-positive, Gram-negative bacteria, and the yeast-like pathogenic fungus Candi

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35

Valenta, Vladimír, Hana Hulinská, Jiří Holubek, et al. "N-substituted derivatives of 6,11-dihydrodibenzo[b,e]thiepin-11-amine and related compounds; Synthesis and pharmacological screening." Collection of Czechoslovak Chemical Communications 53, no. 4 (1988): 860–69. http://dx.doi.org/10.1135/cccc19880860.

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Reactions of N-(6,11-dihydrodibenzo[b,e]thiepin-11-yl)chloroacetamide (II) with dimethylamine, morpholine, and 2-(1-piperazinyl)ethanol afforded the amino amides III-V. Substitution reactions of 11-chloro-6,11-dihydrodibenzo[b,e]thiepin with ethylenediamine and N,N-dimethylethylenediamine gave the diamines VI and VII. 6,11-Dihydrodibenzo[b,e]thiepin-11-amine (I) was treated with ethyl chloroacetate and ethyl 2-bromopropionate to give the amino esters X and XI which were transformed on the one hand to the acids VIII and IX, and to the amides XII and XIII on the other. (6,11-Dihydrodibenzo[b,e]t

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36

Reginato, Gianna, Maria Pia Catalani, Alessandro Mordini, et al. "Stereoselective cyclopropanation of chiral 5-substituted dihydro-2H-piperazines." Tetrahedron: Asymmetry 24, no. 1 (2013): 75–79. http://dx.doi.org/10.1016/j.tetasy.2012.11.015.

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37

Patil, Pravin, Rudrakshula Madhavachary, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, and Alexander Dömling. "De Novo Assembly of Highly Substituted Morpholines and Piperazines." Organic Letters 19, no. 3 (2017): 642–45. http://dx.doi.org/10.1021/acs.orglett.6b03807.

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38

Nurgatin, V. V., B. M. Ginzburg, V. I. Kovalenko, and G. A. Marchenko. "Acidic fission of 1,4-diformyl-2,3,5,6-tetra substituted piperazines." Chemistry of Heterocyclic Compounds 21, no. 9 (1985): 1057. http://dx.doi.org/10.1007/bf00515035.

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39

Berkheij, Martin, Lisan van der Sluis, Claudia Sewing та ін. "Synthesis of 2-substituted piperazines via direct α-lithiation". Tetrahedron Letters 46, № 14 (2005): 2369–71. http://dx.doi.org/10.1016/j.tetlet.2005.02.085.

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MATSUMOTO, K., S. HASHIMOTO, M. TODA, M. HASHIMOTO, and S. OTANI. "ChemInform Abstract: Synthesis of Unsymmetrically 1,4-Heteroaryl-Substituted Piperazines." ChemInform 23, no. 2 (2010): no. http://dx.doi.org/10.1002/chin.199202234.

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Chatterjee, N. R., B. G. Chandak, G. R. Jadhav, and D. C. Sharma. "Synthesis and Anti-Anxiety Activity of Some 1-Piperazino Derivatives of 2, 4-Diphenyl 2, 3-Dihydro-1, 5-Benzodiazepine." International Journal of Drug Design and Discovery 1, no. 2 (2010): 136–39. https://doi.org/10.37285/ijddd.1.2.4.

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Halogenation reaction of 2-methyl, 2, 4- diphenyl-1H-1, 5-benzodiazepine (1) with thionyl chloride gave the N-chloro derivative(2) which on condensation with 4- substituted piperazines afforded the title compounds (3) which were characterized by analytical and spectral data. All these compounds (3a-c) showed significant anti-anxiety activity against diazepam as a standard by elevated plus maze method.

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Kirschning, Andreas, Heiko Sommer, Max Braun, and Benjamin Schröder. "4-Ethoxy-1,1,1-trifluoro-3-buten-2-one (ETFBO), a Versatile Precursor for Trifluoromethyl-Substituted Heteroarenes – a Short Synthesis of Celebrex® (Celecoxib)." Synlett 29, no. 01 (2017): 121–25. http://dx.doi.org/10.1055/s-0036-1589097.

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4-Ethoxy-1,1,1-trifluoro-3-buten-2-one (ETFBO) serves as a trifluoromethyl-containing building block for the preparation of trifluoromethyl-substituted thiophenes, furans, pyrrols, and piperazines. Key steps are an addition–elimination reaction to ETFBO followed by the thiazolium-catalyzed Stetter reaction. The scope of this chemistry was demonstrated in a new synthetic approach towards the COX-2 selective, nonsteroidal anti-inflammatory drug Celebrex® (celecoxib).

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Kozlowski, Joseph A., Guowei Zhou, Jayaram R. Tagat, et al. "Substituted 2-(R)-Methyl piperazines as muscarinic M2 selective ligands." Bioorganic & Medicinal Chemistry Letters 12, no. 5 (2002): 791–94. http://dx.doi.org/10.1016/s0960-894x(02)00023-9.

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Tierney, Elizabeth J., Anthony D. Sabatelli, and Joseph E. Sarneski. "Stereochemical preferences of methyl-substituted piperazines chelated to platinum(II)." Inorganic Chemistry 26, no. 4 (1987): 617–20. http://dx.doi.org/10.1021/ic00251a025.

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Abe, Takashi, Hajime Baba, and Irina Soloshonok. "Electrochemical fluorination of several 1,4-bis[(methoxycarbonyl)alkyl] substituted piperazines." Journal of Fluorine Chemistry 108, no. 2 (2001): 215–28. http://dx.doi.org/10.1016/s0022-1139(01)00357-8.

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Klochkova, I. N., N. N. Semenova, A. A. Safonova, and M. V. Noritsina. "Search for potential cholinesterase inhibitors among substituted pyrrolidines and piperazines." Pharmaceutical Chemistry Journal 33, no. 12 (1999): 638–41. http://dx.doi.org/10.1007/bf02974938.

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Zhai, Huimin, Andrey Borzenko, Ying Yin Lau, Shin Hye Ahn, and Laurel L. Schafer. "ChemInform Abstract: Catalytic Asymmetric Synthesis of Substituted Morpholines and Piperazines." ChemInform 44, no. 21 (2013): no. http://dx.doi.org/10.1002/chin.201321195.

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Al-Soud, Yaseen A., Haitham Al-Sa’doni, Houssain A. S. Amajaour, and Najim A. Al-Masoudib. "Nitroimidazoles, Part 3. Synthesis and anti-HIV Activity of New N-Alkyl-4-nitroimidazoles Bearing Benzothiazole and Benzoxazole Backbones." Zeitschrift für Naturforschung B 62, no. 4 (2007): 523–28. http://dx.doi.org/10.1515/znb-2007-0406.

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A series of 4-nitroimidazole derivatives bearing substituted piperazines (5, 8, 9, 12, 14, 16, 17, and 19 - 21) were synthesized with the aim to develop new non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. All compounds are inactive, except compound 21 which showed inhibition of HIV-1 with EC50 0.20 μg/mL, and therapeutic indexes (SI) of 12.

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İbiş, Cemil, F. Gülay Kirbaşlar, and Gökşin Aydinli. "SOME NEW S-, S,S- AND N,S-SUBSTITUTED 2-NITRODIENES AND BUTADIENYL-SUBSTITUTED PIPERAZINES." Phosphorus, Sulfur, and Silicon and the Related Elements 179, no. 10 (2004): 1975–82. http://dx.doi.org/10.1080/10426500490467101.

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Casalone, Enrico, Tiziano Vignolini, Laura Braconi, et al. "Characterization of substituted piperazines able to reverse MDR in Escherichia coli strains overexpressing resistance-nodulation-cell division (RND) efflux pumps." Journal of Antimicrobial Chemotherapy 77, no. 2 (2021): 413–24. http://dx.doi.org/10.1093/jac/dkab388.

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Abstract Background MDR in bacteria is threatening to public health. Overexpression of efflux pumps is an important cause of MDR. The co-administration of antimicrobial drugs and efflux pump inhibitors (EPIs) is a promising approach to address the problem of MDR. Objectives To identify new putative EPIs and to characterize their mechanisms of action. Methods The effects of four selected piperazine derivatives on resistance-nodulation-cell division (RND) pumps was evaluated in Escherichia coli strains overexpressing or not expressing RND pumps by assays aimed at evaluating antibiotic potentiati

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