DerivativesCompoundsCharacterizationMethyl2021Molecules2019Moiety20202023EVALUATION2017Small moleculeSolid-phase synTriethylamineAmidesNitrogenCommercially availablePrecursorsDerivativeNucleusPeptidePsychoactiveOrganic ChemistryBenzylAcidAnaloguesReactionSeriesChlorideEfficientInvestigationCompoundAssayZincDrugYieldApplicationChemical
Derivatives5
- The present review focuses on the synthesis and application of different piperazine derivatives and their metal complexes having diverse applications. (rsc.org)
- The Tungsten-Promoted Synthesis of Piperidyl-Modified erythro-Methylphenidate Derivatives. (acs.org)
- We reported the syntheses of novel cinnamide derivatives containing bis(4-fluorophenyl)methyl moiety starting from commercially available materials. (scielo.org.za)
- The invention relates to 1-piperazine- and 1-homopiperazine-carboxylate derivatives, and to the preparation and therapeutic application thereof. (allindianpatents.com)
- Design, synthesis, biological evaluation, and molecular modeling of coumarin-piperazine derivatives as acetylcholinesterase inhibitors. (journals.cz)
Compounds9
- The piperazine scaffold is a privileged structure frequently found in biologically active compounds. (rsc.org)
- This is one of the reasons why piperazine based compounds are gaining prominence in today's research. (rsc.org)
- Piperazine ring-based compounds find their application in biological systems with antihistamine, anticancer, antimicrobial and antioxidant properties. (rsc.org)
- Thus, linking together a pyridine π-system and a cyclic amine moiety via a piperazine ring affords compounds with low affinity, but good selectivity for α4β2 * nicotinic receptors. (uky.edu)
- Herein, to achieve efficient delivery of negatively charged siRNA duplexes, the internal cavity of "humanized"chimeric Archaeal ferritin (HumAfFt) was specifically decorated with novel cationic piperazine-based compounds (PAs). (unicatt.it)
- Cinnamic acids are one of the key intermediates for the synthesis of this series of compounds, which are usually obtained by the Perkin reaction, 8 the Knoevenagel condensation, 9 the Claisen condensation, 10 and the Heck reaction. (scielo.org.za)
- Pyrrolidine as an organocatalyst enables a general and efficient biomimetic method for the synthesis of aldimines from aldehydes and compounds bearing an amino group. (organic-chemistry.org)
- In this research, we tested five compounds owned by a novel group of piperazine arylideneimidazolones for the capability to inhibit the AcrAB-TolC efflux pump. (technumber.com)
- A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. (justia.com)
Characterization2
- Synthesis, characterization and analysis of physico-chemical properties of 1H-indol-5-yl-[4-(2-phenoxyethyl)piperazin-1-yl]methanone', Završni rad, Sveučilište u Zagrebu, Fakultet kemijskog inženjerstva i tehnologije, citirano: 25.11.2023. (unizg.hr)
- R. Devine, D. S. D. Martin, G. K. Kinsella, J. B. C. Findlay, J. C. Stephens (2020) 'Characterization of an aryl piperazine/ 2-hydroxypropyl-β-cyclodextrin association, a complex with antidiabetic potential' . (maynoothuniversity.ie)
Methyl12
- The title compound (E)-1-{4-[bis(4-methoxyphenyl)methyl]piperazin-1-yl}-3-(4-chloro- phenyl)prop-2-en-1-one (C 28 H 29 ClN 2 O 3 , Mr = 476.98) (5) was synthesized and studied by the single crystal X-ray diffraction method. (scielo.org.za)
- The reaction of cinnamic acid chloride with 1-[bis(4-methoxyphenyl)methyl]piperazine in the presence of triethylamine in dichloromethane at room temperature afforded the corresponding new cinnamide derivative with a total yield of 73.5 % ( Scheme 1 ), which was expected to be a potent neuroprotective agent. (scielo.org.za)
- 7 In this article, we present our results on the synthesis, crystal structure and anti-ischaemic activity of new cinnamide derivative of (E)-1-{4-[bis(4-methoxyphenyl)methyl]piperazin-1- yl}-3-(4-chlorophenyl)prop-2- en-1-one (5). (scielo.org.za)
- E)-1-{4-[bis(4-methoxyphenyl)methyl]piperazin-1-yl}-3-(4-chlorophenyl)prop-2-en-1-one (5). (scielo.org.za)
- 13 The title compound (E)-1-{4-[bis(4-methoxyphenyl)methyl]piperazin-1-yl}-3-(4-chlorophenyl)prop-2-en-1-one 5 was obtained as follows:thionylchloride (2mL) and piperadine (1 drop) were added to a stirred solution of (E)-3-(4-chlorophenyl)acrylic acid (4,4 mmol) in dichloromethane (15 mL) at room temperature. (scielo.org.za)
- The design of the ligand is based upon 1-(3', 4'-dimethoxyphenethyl)-4-(3''-phenylpropyl) piperazine (1), a sigma1 agonist developed by Santen Pharmaceutical Co. Through a three-step synthesis, we have replaced one of the methyl groups with a diaminedithiol (DADT) chelating moiety attached through an alkyl chain (2). (umsystem.edu)
- A new series of 7-fluoro-6-(4-methyl-1-piperazinyl)-2-(thiosubstituted)- 4(3H)-quinazolinones was synthesized as potential antitumor agents by multi-step synthesis starting with the commercially available 3-chloro-4-fluoroaniline. (elsevierpure.com)
- Find complete chemical information for 1-(METHYL-D3)PIPERAZINE 2HCL . (clearsynth.com)
- 1-(Methyl-D3)piperazine 2HCl, a remarkable chemical compound, is characterized by its deuterium-labeled methyl group and its association with piperazine, a bicyclic heterocyclic amine. (clearsynth.com)
- 1-(METHYL-D3)PIPERAZINE 2HCL in Bulk is primarily used in Pharmaceutical Industry and Drug Discovery. (clearsynth.com)
- This page contains information about 1-(METHYL-D3)PIPERAZINE 2HCL. (clearsynth.com)
- You can buy 1-(METHYL-D3)PIPERAZINE 2HCL from Clearsynth at best competitive price with assured price guarantee. (clearsynth.com)
20211
- 2021 ) Design and Synthesis of Highly Potent and Specific ABHD6 Inhibitors. (academictree.org)
Molecules3
- In addition to the ring carbons, substitution in the nitrogen atom of piperazine not only creates potential drug molecules but also makes it unique with versatile binding possibilities with metal ions. (rsc.org)
- Piperazine-derived small molecules as potential Flaviviridae NS3 protease inhibitors. (us.es)
- The method that we developed allows a straightforward structural modification of bioactive molecules (e.g., α-amino acids) by the conversion of a primary amino group into a piperazine ring. (bvsalud.org)
20193
- 2019 ) Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors. (academictree.org)
- 2019 ) Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology. (academictree.org)
- Stephens J.C. (2019) 'Cinnamaldehydes: Synthesis, antibacterial evaluation, and the effect of molecular structure on antibacterial activity' . (maynoothuniversity.ie)
Moiety1
- The docking pose of the studied LA1 molecule depends of the protonated state of the nitrogen atom of the piperazine moiety where in the best scored poses, the xanthine moiety of LA1 is bound into the catalytic active site (CAS) of AChE, while the arylpiperazine fragment is placed into the peripheral binding site (PAS). (journals.cz)
20202
- Timothy M. Monos, Jonathan N. Jaworski, John C. Stephens, Timothy F. Jamison (2020) 'Continuous-Flow Synthesis of Tramadol from Cyclohexanone' . (maynoothuniversity.ie)
- 2020) Development and Validation of a GC-MS Method for the Simultaneous Quantification of Two Piperazine Designer Drugs Sold in Combination as 'Legal X'. Ann Toxicol 2(1):15-25. (scholars.direct)
20231
- 2023-08-15 6269-89-2 1-(4-Nitrophenyl)piperazine Distributor. (providechemical.com)
EVALUATION4
- Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2β-carbomethoxy-3β-(4′-halophenyl)nortropanes: Candidate Radioligands for In Vivo Imaging of the Brain Dopamine Transporter with Positron Emission Tomography. (acs.org)
- Synthesis and Biological Evaluation of Bupropion Analogues as Potential Pharmacotherapies for Cocaine Addiction. (acs.org)
- Brandt M, Gammeltoft S, Jensen KJ (2006) Microwave heating for solid-phase peptide synthesis: general evaluation and application to 15-mer phosphopeptides. (springer.com)
- Perich JW, Ede NJ, Eagle S, Bray AM (1999) Synthesis of phosphopeptides by the Multipin method: evaluation of coupling methods for the incorporation of Fmoc-Tyr(PO3Bzl, H)-OH, Fmoc-Ser(PO3Bzl, H)-OH and Fmoc-Thr(PO3Bzl, H)-OH. (springer.com)
20171
- Although these drugs have been massively consumed by the young attenders of electronic music nightclubs and rave parties in Australia, China and UK [ 13 - 17 ], they have also been a abuse drug of choice in other European countries, with the EMCDDA drug report of 2017 stating that piperazines corresponded to 6% of the NPS reported to the EU Early Warning System [ 18 ]. (scholars.direct)
Small molecule1
- Piperazine is one of the most frequently found scaffolds in small-molecule FDA-approved drugs. (bvsalud.org)
Solid-phase syn3
- Garcia-Martin F, Quintanar-Audelo M, Garcia-Ramos Y, Cruz LJ, Gravel C, Furic R, Cote S, Tulla-Puche J, Albericio F (2006) ChemMatrix, a poly(ethylene glycol)-based support for the solid-phase synthesis of complex peptides. (springer.com)
- Lacombe JM, Andriamanampisoa F, Pavia AA (1990) Solid-phase synthesis of peptides containing phosphoserine using phosphate tert. (springer.com)
- Otvos L Jr, Elekes I, Lee VM (1989) Solid-phase synthesis of phosphopeptides. (springer.com)
Triethylamine1
- Obtained sulfonate ester was further substituted with piperazine using triethylamine as base. (unizg.hr)
Amides1
- Bernatowicz M, Daniels S, Koster H (1989) A comparison of acid labile linkage agents for the synthesis of C-terminal amides. (springer.com)
Nitrogen1
- In this study, a general approach to the synthesis of piperazines bearing substituents at carbon and nitrogen atoms utilizing primary amines and nitrosoalkenes as synthons was developed. (bvsalud.org)
Commercially available3
- 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. (rsc.org)
- All chemicals, reagents, and solvents for synthesis of the compound were commercially available and used without further purification. (scielo.org.za)
- First step in synthesis included making a good leaving group from commercially available alcohol by nucleophilic substitution with mesyl-chloride. (unizg.hr)
Precursors3
- From the benzyl protected precursors, the 2-substituted piperazines bearing a Boc-protecting group could consequently also be obtained via a simple protection and deprotection step of the corresponding piperazines. (rsc.org)
- Cu(ethylxanthate)$_2$, Cu(morpholine-4-dithiocarbamate)$_2$ and Cu(piperazine-1-dithiocarbamate)$_2$ are used as efficient single source precursors for the synthesis of CuS NSs. (ias.ac.in)
- Synthesized NSs crystalize in hexagonal crystal structure, having average crystallite size ${\sim}$28.95, 32.85 and 33.30 nm for CuS prepared from Cu(ethylxanthate)$_2$, Cu(morpholine-4-dithiocarbamate)$_2$ and Cu(piperazine-1-dithiocarbamate)$_2$ precursors, respectively. (ias.ac.in)
Derivative1
- This unique isotopically labeled derivative of piperazine holds significant importance in various scientific and pharmaceutical applications. (clearsynth.com)
Nucleus1
- Piperazine nucleus is found in many marketed drugs in the realm of antidepressants (amoxapine), antipsychotics (bifeprunox), antihistamines (cyclizine and oxatomide), antifungals (itraconazole), antibiotics (ciprofloxacin), etc . (rsc.org)
Peptide3
- The formation of 3-(1-piperidinyl)alanyl-containing peptides via phosphoryl β -elimination was identified from the application of Fmoc-Ser(PO 3 Bzl,H)-OH in peptide synthesis as shown by RP-HPLC, ES-MS and 31 P-NMR analysis. (springer.com)
- An examination of alternative bases for the minimization of byproduct formation showed that cyclohexylamine, morpholine, piperazine and DBU gave complete suppression of β -elimination, with a 50% cyclohexylamine/DCM (v/v) deprotection protocol providing the crude peptide of highest purity. (springer.com)
- In: Pennington MW, Dunn BN (eds) Peptide synthesis protocols. (springer.com)
Psychoactive2
- Fipexide (Attentil, Vigilor) is a psychoactive drug of the piperazine chemical class which was developed in Italy in 1983. (wikipedia.org)
- Recently, the synthesis and abuse of new psychoactive substances (NPS), including the so-called designer drugs, have greatly increased [ 1 ]. (scholars.direct)
Organic Chemistry1
- Research in the Stephens Group is focused on the discovery and application of new technologies such as continuous flow, new reactions, and new catalysts in organic synthesis, as well as applications of organic chemistry at the interface of chemistry & biology. (maynoothuniversity.ie)
Benzyl1
- A straightforward synthesis of a variety of 1,4-bis-benzylpiperazines from benzyl halides and 2-bromoethylamine hydrobromide is described. (tcnj.edu)
Acid1
- In the final step of synthesis, obtained intermediate reacted with indole-5-carboxylic acid accordingly to the Steglich mechanism of amidation using DMAP as the catalyst. (unizg.hr)
Analogues1
- Synthesis of analogues showing activity in in vitro assay on Kv1.5 potassium ion channel was described in the literature, which is validated biological target in the treatment of arrhythmia. (unizg.hr)
Reaction1
- Compound V , obtained by a reaction of 2-chloro-4'-fluoroacetophenone with 1-(ethoxycarbonyl)piperazine, was reduced with sodium borohydride to the amino alcohol VIf . (cas.cz)
Series1
- A series of N,N-disubstituted piperazines were prepared and evaluated for binding to α4β2 * and α7 * neuronal nicotinic acetylcholine receptors using rat striatum and whole brain membrane preparations, respectively. (uky.edu)
Chloride2
- PTC alkylation of piperazine (1) with 2 equivalents of piperonyl chloride [25054-53-9] (2) in the presence of cetrimonium bromide gives 1,4-bis-piperonylpiperazine [55436-41-4] (3). (wikipedia.org)
- The hydrochloride of VIf was treated with thionyl chloride to give the hydrochloride of 1-[2-chloro-2-(4-fluorophenyl)ethyl]-4-(ethoxycarbonyl)piperazine ( VIg ). (cas.cz)
Efficient1
- This protocol is as an efficient alternative to conventional methods for the synthesis of imines and amines. (organic-chemistry.org)
Investigation1
- Synthesis and investigation of a new organic electrode material based on condensation product of triquinoyl with p-phenylenediamine. (ac.ru)
Compound1
- With regards to this result, 1H-indol-5-yl-(4-(2-phenoxyethyl)piperazine-1- yl)methanone is potentially interesting compound for further in vitro profiling of Kv1.5 inhibition. (unizg.hr)
Assay1
- Nile crimson efflux assay in the lack and presence from the piperazine arylideneimidazolone EPIs. (technumber.com)
Zinc1
- The task was to test whether lead, mercury, copper, zinc and benzene in environmentally relevant concentrations influence porphyrin synthesis of cells. (who.int)
Drug3
- The practical utility of this methodology was demonstrated for chiral drug synthesis. (rsc.org)
- The synthesis, crystal structure, absolute configuration, spectroscopic and spectrometric details of topiramate azido-sulfate, a precursor to the anti-convulsant drug topiramate, are presented. (iucr.org)
- In the future, drug discovery experiments utilizing this information could be performed, permitting the synthesis of new drugs with better safety profile. (bvsalud.org)
Yield2
- The catalytic system can also be used for a one-pot synthesis of imines in excellent yield. (organic-chemistry.org)
- In addition, alternative synthesis was proposed with the aim to increase overall yield due to possible application for the scale-up synthesis. (unizg.hr)
Application1
- The application of the alternative N α -deprotection protocol using 50% cyclohexylamine/DCM (v/v) is therefore recommended for deprotection of the Fmoc group from the Fmoc-Ser(PO 3 Bzl,H) residue, with particular benefit anticipated for the synthesis of multiphosphoseryl peptides. (springer.com)
Chemical1
- Furthermore, the compound's structural features contribute to its versatility in diverse chemical syntheses and analytical techniques, making it a valuable asset in the pursuit of scientific discoveries and advancements in the field of chemistry. (clearsynth.com)