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2.2 General Synthetic Methods of Piperazine derivatives:

FIG.1: SYNTHESIS OF 1, 4-BIS-(4-DIMETHYL AMINO BENZYL)-PIPERAZINE-2, 3-DIONE

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Synthesis of morpholine or piperazine derivatives …

Negus, S.S., Baumann, M.H., Rothman, R.B., Mello, N.K., Blough, B.E. (2009), ‘Selective Suppression of Cocaine- versus Food-Maintained Responding by Monoamine Releasers in Rhesus Monkeys: Benzylpiperazine, (+)Phenmetrazine, and 4-Benzylpiperidine’, , Volume 329, pp. 272–281.

Physical data for the N-(2,3-dimethylphenyl)-N’-(aryl-diazenyl)-piperazines (3).

CONCLUSION: Compared to two different schemes, the compound produced by scheme: PZ-1 got more yield value. Among them PZ-2 yield percentage was high, 80.8%. Scheme 2 had good yield value but took comparatively longer time of reaction as it produced complex or higher molecular weight piperizine derivatives. It proves that ethylene diamine is the good precursor for synthesizing piperazine and its derivatives.

piperazine derivatives(Fig.17) synthesis ..

Physical data for series of 1-(4-methylbenzyl)-4-(aryldiazenyl)-piperazines (4).

The reaction mixture was left over night and the separated solid product was obtained by filtration and dried. The crude drug was re-crystallized from ethanol affording 1, 4-Bis-(4-dimethyl amino benzyl)-piperazine-2,3-dione.

The synthesized compounds (PZ1-PZ5) were evaluated in vitro for their antihelmintic activities according to the protocol mentioned below. The earthworms were collected from fish farm, Tararha. Sunsari, Nepal and species identification was done from Biology Department of Central Campus of Technology, Hattisar, Dharan, Nepal.

Synthesis and Antimicrobial Activity of Piperazine Derivatives

As mention above that various literatures of piperazine signifies N-phenyl /alkyl or bisaryl/benzyl derivatives are found possess various pharmacological and biological activities here the work is aimed to synthesis some bis benzyl (containing N-methyl group)derivatives of piperazine in one hand and benzimidazole linked piperazine derivatives in other hand and compare their antihelminthic activities.

Animal studies have demonstrated that BZP stimulates the release and inhibits the reuptake of , and . BZP appears to be metabolised by cytochrome P450 (possibly involving the CYP2D6 iso-enzyme) and catechol-O-methyl-transferase (COMT). These systems are prone to genetic polymorphisms, so potential inter-individual differences may occur. In animal and human studies, the main metabolites are 4-hydroxy-BZP, 3-hydroxy-BZP, 4-hydroxy-3-methoxy-BZP, piperazine, benzylamine and N-benzylethylenediamine. The hydroxy-metabolites are also excreted as glucuronic and/or sulphuric acid conjugates in urine.

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  • Piperazine synthesis - Organic chemistry

    Physical data for series of 1-(2-methylbenzyl)-4-(aryldiazenyl)-piperazines (5).

  • A practical method allows the synthesis of alkyl-, ..

    Physical data for series of 1-(3-methylbenzyl)-4-(aryldiazenyl)-piperazines (6).

  • Synthesis and antimicrobial activity of N-alkyl and N …

    Physical data for Methyl 4-[2-(4-phenethylpiperazino)-1-diazenyl]benzoate (7).

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Patent US2809196 - Synthesis of piperazine - Google …

A series of six piperazine like derivatives of 3,7-dimethylxanthine (theobromine) was synthesized. The structures of the new compounds were confirmed by IR and 1H NMR. The results were consistent with the assigned structures. All compounds were in vitro screened for their activity as antioxidants. It was established that the difference in the chemical structure of the compounds reflects to their relative ability to quench aqueous peroxyl radicals and to reduce the ABTS+, DPPH free radical and ferric ion in in vitro systems. For the three discussed methods, the highest antioxidant activity was demonstrated by compound 3c. The antioxidant activity of the studied compounds against lipid peroxidation was also measured. No significant inhibition of lipid peroxidation compared to the control has been observed for the set of compounds, except for compound 3c, which demonstrated the highest significant diminution of linoleic acid with an effect comparable with the BHT effect, used as a control. From the performed evaluations, we may conclude that the presence of a hydroxyl group in the structure is essential for the antioxidant properties and should be taken into consideration in further design of structures with potential antioxidant properties.

07/06/2017 · ARTICLE

In this paper, we apply four common methods [] for the determination of free radicals scavenging activity, total antioxidant capacity and antioxidant activity against lipid peroxidation to both lipophilic and hydrophilic antioxidants in an attempt to establish the most appropriate one for evaluation of possible antioxidant effects, demonstrated from the newly synthesized arylpiperazine derivatives. The described methods were chosen for their user-friendly mechanisms for antioxidant activity determination since they require a simple machine like a spectrophotometer, which is commonly available in most laboratories.

Synthesis and various properties of piperazine by …

ABSTRACT: The broad and potent activity of piperazine has established it as one of the biologically important scaffolds. This article is an effort to highlight the importance of the piperazine in the present context and promise they hold for the future. This review mainly focused the updated information on the most active piperazine derivatives that have been reported to show significant biological actions for instance anti-microbial, anti-depressant, anticonvulsant, anti-parkinson, anti-inflammatory, antipsychotic, antioxidant, antidiabetic, antiarrhythmic, antiproliferative, anxiolytic, antialzheimer, antimalarial, antihypertensive, antiplatelet aggression and anti-histaminic activity. This review would take on benzylpiperazine (BZP) and trifluoromethylpiperazine (TFMPP), benzhydryl piperazine, diphenylalkyl piperazine, phenyl piperazine as the most popular member of the piperazines, focusing the discussion on their origins, pharmacokinetics and pharmacodynamics, and their effects on the human body. From these outcomes, information for future molecular modifications leading to compounds with greater positive pharmacological properties may be derived.

Piperazine & Derivatives - CDH Fine Chemical

More detailed information about the structure of compounds 3a–f was provided by the 1H NMR spectra. The 1H NMR spectra of the compounds 3a–f showed the signals of the respective protons of the synthesized compounds, which were verified on the basis of their chemicals shifts, multiplicities and coupling constants. Thus, the strong singlets at 3.48.58 and 3.89.99 ppm in the spectrum of the studied compounds correspond to N-methyl protons at positions 3 and 7. The signal of the proton at position 8 appears at 7.50.54 ppm as strong singlet. The signals of methylene protons from the benzyl side chain at position 1 form strong singlet at 4.80 ppm. The signals of the aromatic protons from substituted benzyl side chain in the spectra of 3b–e correspond to complicated multiplets between 6.82 and 6.97 ppm, while the same protons in unsubstituted benzyl moiety (3a) appear as multiplet 7.27 and 7.37 ppm. The aromatic protons in benzhydryl group in 3f form multiplet at 7.27 and 7.35 ppm. The methylene proton from the benzhydryl residue forms a singlet with weak to medium intensity at 4.36 ppm. The integral curves correspond to the exact number of the protons. The values of the chemical shifts of the protons registered by 1H NMR spectra were compared with simulated values.[] Due to an impossibility to render an account of influence of the solvent, we observed only small deviations of the computed values from the experimental values. Regardless, the simulated 1H NMR spectra are in good correlation with experimental ones.

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