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PiperazinesAscarisBuspironeDesigner DrugsReceptors, sigmaSerotonin Receptor AgonistsAntinematodal AgentsMolecular StructureReceptors, SerotoninStereoisomerismPyronineStructure-Activity RelationshipMitragynaProchlorperazineSerotonin AntagonistsReceptors, Serotonin, 5-HT1Cyclization8-Hydroxy-2-(di-n-propylamino)tetralinProtein BiosynthesisTrazodoneCatatoniaN-Methyl-3,4-methylenedioxyamphetamineDopamine Uptake InhibitorsDelavirdineReceptors, Dopamine D3PiperidinesDose-Response Relationship, DrugAnthelminticsSerotoninProtein Synthesis InhibitorsPyrantelRadioligand AssayAscariasisSerotonin 5-HT1 Receptor AgonistsKineticsTrimetazidineRNA, MessengerReceptor, Serotonin, 5-HT1AReceptors, Dopamine D2Dopamine Plasma Membrane Transport ProteinsIsocyanatesRats, Sprague-DawleyTetrahydronaphthalenesBisbenzimidazoleMagnetic Resonance SpectroscopyAnti-Anxiety AgentsMonoacylglycerol Lipases3,4-MethylenedioxyamphetamineCells, CulturedMolecular Sequence DataDiethylcarbamazineEscherichia coliDrug InteractionsCycloheximideDNAMolecular ConformationDopamineDNA ReplicationEnzyme InhibitorsTime FactorsBase SequenceRats, WistarCell LineMutationBiogenic MonoaminesTritiumRats, Inbred StrainsAlkylationLigandsLeucineBinding, CompetitiveMembrane Transport ProteinsChromatography, High Pressure LiquidTranscription, GeneticMicrosomes, LiverCarbon IsotopesMuscle TonusRNACocaineMass SpectrometryLiverDactinomycin1-(5-Isoquinolinesulfonyl)-2-MethylpiperazineCell-Free SystemAnti-Bacterial AgentsBacterial ProteinsChemistry Techniques, SyntheticReceptor, Serotonin, 5-HT2AGas Chromatography-Mass SpectrometryMotor ActivityMusclesModels, MolecularProtein BindingPuromycinThymidineAmino Acid SequenceChromatography, LiquidPeptide BiosynthesisMicrobial Sensitivity TestsIsoquinolines
DerivativesCompoundsAryl piperazinesCharacterizationEvaluationMoleculesMoietyHeterocyclicPharmacological2HCLIntermediatesDerivativeAntidepressantsVitroNitrogenInhibitoryHydroxylationChemistrySmall-moleculeDesignDiscoveryBenzylMelaninInhibitorsQuinolineStructuralEnzyme2020CompoundUrinePharmaceutical IndustryReactionsAminoPsychoactiveLipophilicConcentrationsInteractionsAcidResearchActivityAntibioticSeriesStimulationApplicationDevelopmentPotential drugWarningsFound
Derivatives5
  • The present review focuses on the synthesis and application of different piperazine derivatives and their metal complexes having diverse applications. (rsc.org)
  • Design, synthesis, biological evaluation, and molecular modeling of coumarin-piperazine derivatives as acetylcholinesterase inhibitors. (journals.cz)
  • The Tungsten-Promoted Synthesis of Piperidyl-Modified erythro-Methylphenidate Derivatives. (acs.org)
  • The present research work involved synthesis of some novel pyridazine derivatives and evaluation of their analgesic and anti-inflammatory activities in experimental animals to obtain safer non-steroidal anti-inflammatory drugs (NSAIDs). (ugm.ac.id)
  • 2012, Design, Synthesis and Evaluation of Anti-inflammatory and Ulcerogenecity of Novel Pyridazinone Derivatives, Med. (ugm.ac.id)
Compounds8
  • 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)
  • All designed compounds showed comparable affinity to the catalytic site of the enzyme to that of the standard drug, however, the activity as inhibitors, as reflected by the IC 50 range of 0.3 μM - 1.3 μM, was lower than that of Sitagliptin (IC 50 22 nM). (ommegaonline.org)
  • Guided by molecular modeling, the six designed compounds were docked into DPP-IV catalytic sites to identify their binding poses and compare it with the standard drug pose in the crystal structure. (ommegaonline.org)
  • All the title compounds except compound 5 are predicted to be safe by Osiris online software and are likely to have good oral bioavailability as they obey Lipinski's rule of five for drug likeness. (ugm.ac.id)
  • The compounds synthesized contain triazole ring directly connected to an aromatic ring or via a piperazine linker. (pdx.edu)
Aryl piperazines1
  • Modeling studies demonstrate that aryl piperazines ( I ), Aryloxyalkylamines ( II ), phenylalkykamines ( III ) and indolylalkylamines ( VI ) might interact at 5-HT receptors in a similar manner. (healthdrugpdf.com)
Characterization3
  • Here we describe the synthesis, pharmacological, and in silico characterization of a novel arylpiperazines series with excellent 5-HT1A affinity. (ac.rs)
  • 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)
  • 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)
Evaluation3
  • Stephens J.C. (2019) 'Cinnamaldehydes: Synthesis, antibacterial evaluation, and the effect of molecular structure on antibacterial activity' . (maynoothuniversity.ie)
  • 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)
Molecules5
  • 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)
  • The accentuated molecules could serve as a lead compound for developing 5-HT1A drug-like molecules for depression treatment. (ac.rs)
  • The current research aimed to design molecules maintaining the β-amino amide pharmacophore of Sitagliptin, but with the triazolo-piperazine ring system replaced by more lipophilic entities for better hydrophobic interactions with Phe 357 in the S2 pocket. (ommegaonline.org)
Moiety2
  • In most antidepressants, a piperazine-based structural motif can be identified as a common moiety. (ac.rs)
  • 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)
Heterocyclic2
  • 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)
  • In addition to offering an attractive collection of heterocyclic building blocks and fragments, Avistron also offers bespoke services in the areas of intermediate and library compound synthesis. (avistronchemistry.com)
Pharmacological5
  • Synthesis of novel 5-HT1A arylpiperazine ligands: Binding data and computer-aided analysis of pharmacological potency. (ac.rs)
  • Its incorporation of deuterium atoms allows for precise tracing and elucidation of metabolic pathways, making it invaluable in pharmacological research and drug development. (clearsynth.com)
  • Alnavas - Pharmacological action Alnavas is a lipid-lowering drugs of the statin group. (medicatione.com)
  • Alur - Pharmacological action Alur is a medication that violates the synthesis of uric acid. (medicatione.com)
  • Cipromep - Pharmacological action Cipromep is a broad-spectrum antimicrobial drug of fluoroquinolone group with bactericidal action. (medicatione.com)
2HCL4
  • Find complete chemical information for 1-​(METHYL-​D3)​PIPERAZINE 2HCL . (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)
Intermediates4
  • N-dealkylation followed by hydroxylation of the piperazine ring is proposed to cause the bioactivation to iminium intermediates captured by cyanide. (bvsalud.org)
  • Experimental and theoretical analyses led to the identification of two key intermediates en route to DHPs and the explanation of the observed regioisomeric ratios. (ac.rs)
  • We have successfully completed a large number of orders for chemical custom synthesis on timeOur company is committed to the research and development, production and sales of bulk drugs and their intermediates, fine chemicals.The production base is mainly located in Liaocheng City, Shandong Province, and Yuncheng City, Shanxi Province. (nbinno.com)
  • We offer an extensive range of innovative and novel intermediates of high purity for sale in a variety of pack sizes to suit your needs as well as custom synthesis if required. (avistronchemistry.com)
Derivative1
  • This unique isotopically labeled derivative of piperazine holds significant importance in various scientific and pharmaceutical applications. (clearsynth.com)
Antidepressants1
  • 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)
Vitro3
  • The current research addresses the design, modeling, synthesis and in vitro testing of potential new DPP-IV inhibitors. (ommegaonline.org)
  • 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)
  • 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)
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)
Inhibitory1
  • It has however been suggested that meclizine only has an inhibitory effect under normal viewing-circumstances, as the drug has been shown to enhance an isolated vestibular response. (wikipedia.org)
Hydroxylation1
  • The major identified metabolic pathways are oxidation and degradation of the imidazole and piperazine rings, oxidative Odealkylation and aromatic hydroxylation. (nih.gov)
Chemistry4
  • 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)
  • 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)
  • Through a structured PhD programme we provide an excellent in-depth training in organic synthesis and in the interdisciplinary space between chemistry & biology. (maynoothuniversity.ie)
  • Dr. Patil became Research Assistant professor in 2010 and established drug design and discovery research driven by medicinal chemistry at UTHSC. (rosalindfranklin.edu)
Small-molecule1
  • Piperazine is one of the most frequently found scaffolds in small-molecule FDA-approved drugs. (bvsalud.org)
Design2
  • Acetylcholinesterase (AChE) is a good target in the design of new drugs for the treatment of Alzheimer's disease. (journals.cz)
  • Dipeptidyl peptidase-IV enzyme is one of the targets for drug design to compact type-2 diabetes. (ommegaonline.org)
Discovery4
  • In the future, drug discovery experiments utilizing this information could be performed, permitting the synthesis of new drugs with better safety profile. (bvsalud.org)
  • Additional early-stage research and drug discovery news in brief. (bioworld.com)
  • Drug Discovery Today , 26 (12). (maynoothuniversity.ie)
  • Our team has worked successfully with both pharmaceutical and biotech companies to provide products that make a real impact to drug discovery programmes. (avistronchemistry.com)
Benzyl2
  • 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)
  • 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)
Melanin1
Inhibitors3
  • The currently known drugs -donepezil, galantamine and rivastignime- act as moderate AChE inhibitors. (journals.cz)
  • However, drug resistance to these inhibitors is developed resulting in only short-term improvement of patients' survival 15 . (nature.com)
  • DPPIV inhibitors are relatively new class of drugs introduced to the market for the treatment of type2 diabetes. (ommegaonline.org)
Quinoline1
  • It can replace organic base such as triethylamine, N, N - dimethyl aniline, pyridine and quinoline, widely used in organic synthesis and semi-synthetic antibiotic, can offers a satisfactory effect in dehydrohalogenation reaction. (bolivianosglobales.com)
Structural1
Enzyme2
  • Ketoconazole blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14α-demethylase responsible for the conversion of lanosterol to ergosterol in the fungal cell membrane. (nih.gov)
  • The essential enzyme CYP121 is a target for drug development against antibiotic resistant strains of Mycobacterium tuberculosis. (uchile.cl)
20201
  • Timothy M. Monos, Jonathan N. Jaworski, John C. Stephens, Timothy F. Jamison (2020) 'Continuous-Flow Synthesis of Tramadol from Cyclohexanone' . (maynoothuniversity.ie)
Compound1
  • Hence the leaf extract is proved the herbal use of cytotoxic activity and it is recommended as anti-cancer drug further to isolate the bioactive compound and drug designing. (iajpr.com)
Urine1
  • About 13% of the dose is excreted in the urine, of which 2 to 4% is unchanged drug. (nih.gov)
Pharmaceutical Industry1
  • In the pharmaceutical industry, it can be used to synthesize the important drugs for the treatment of coronary heart disease, lactic acid, Xintongping and Xintongping, and to synthesize meclofenac and cinnamon piperazine to make "Xinkean", local anesthetics, fungicides, and hemostasis Medicine etc. (spiritusbrand.com)
Reactions3
  • It is widely used in the production of semi-synthetic cephalospor antibiotic drugs, i.e. under the presence of DBU, ammonia and dichloroethane can produce piperazine in the reactions. (bolivianosglobales.com)
  • For detection of adverse drug reactions, clinical trials usually provide limited information as they are conducted under strictly controlled conditions. (openpharmaceuticalsciencesjournal.com)
  • Some of the adverse drug reactions can be detected only after long term use in larger population and in specific patient groups due to specific concomitant medications or disease. (openpharmaceuticalsciencesjournal.com)
Amino1
  • X-ray structure of Sitagliptin with DPP-IV indicated hydrophobic interaction of the triazolo-piperazine ring system with the S2 pocket through the amino acid Phe357. (ommegaonline.org)
Psychoactive1
  • Recently, the synthesis and abuse of new psychoactive substances (NPS), including the so-called designer drugs, have greatly increased [ 1 ]. (scholars.direct)
Lipophilic1
Concentrations3
  • Ketoconazole can cause elevated plasma concentrations of these drugs and may prolong QT intervals, sometimes resulting in life-threatening ventricular dysrhythmias such as torsades de pointes. (nih.gov)
  • Data from some clinical PK/PD studies and drug interaction studies suggest that oral dosing with ketoconazole at 200 mg twice daily for 3 to 7 days can result in an increase of the QT c interval: a mean maximum increase of about 6 to 12 msec was seen at ketoconazole peak plasma concentrations about 1 to 4 hours after ketoconazole administration. (nih.gov)
  • The task was to test whether lead, mercury, copper, zinc and benzene in environmentally relevant concentrations influence porphyrin synthesis of cells. (who.int)
Interactions3
Acid3
  • Main Uses: As a good acid stripping agent in drug synthesis for organic base. (bolivianosglobales.com)
  • DBU sed in the production of semi-synthetic cephalospor antibiotic drugs, Also used in the preparation of acid stripping agent, antirust, top grade corrosion inhibitor, etc. (bolivianosglobales.com)
  • 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)
Research3
  • The method showed high sensitivity, accuracy and precision for the simultaneous detection and quantification of BZP and TFMPP in the three studied matrices and has direct application for the control of drug abuse in humans, post-mortem analysis, and research purposes. (scholars.direct)
  • Since no analytical methods were previously validated for the concomitant analysis and/or quantification of both drugs, and by virtue of the high frequency of the co-administration of both drugs and the expected toxicological impact, it was deemed of greatest significance to develop and validate a GC-MS methodology that enabled the simultaneous quantification of BZP and TFMPP and that was appropriate for clinical, forensic and research purposes. (scholars.direct)
  • Development of drugs acting on h5-HT serotonin subreceptors represents an exciting new area of research as a result of the increasing attention of the involvement of these receptors in psychiatric disorders. (healthdrugpdf.com)
Activity1
  • Moreover, the incorporation of piperazine linker has brought an enhanced antimalarial activity. (pdx.edu)
Antibiotic1
  • Cefupop - Cefupop information Cefupop is a semi-synthetic cephalosporin antibiotic, destined for oral use, which is able to reduce the development of the drug resistant bacteria. (medicatione.com)
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)
Stimulation1
  • The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. (wikipedia.org)
Application1
  • In addition, alternative synthesis was proposed with the aim to increase overall yield due to possible application for the scale-up synthesis. (unizg.hr)
Development2
  • Rhythm Pharmaceuticals Inc. has presented preclinical data on its new drug candidate, RM-718, a next-generation melanocortin MC4 receptor (MC4R) agonist for weekly administration with a potential development path for hypothalamic obesity. (bioworld.com)
  • Google's Scott Penberthy joins the podcast for a visionary discussion that scans the horizon for startling changes artificial intelligence will bring to drug development in the relatively near future. (bioworld.com)
Potential drug1
  • Niosomes are excellent candidate as potential drug delivery system because of their improved drug solubilization, enhanced penetration power, long shelf life and ease of preparation and administration. (openpharmaceuticalsciencesjournal.com)
Warnings1
  • Aleflox warnings This drug belongs in the FDA pregnancy category C. Aleflox may cause severe side effects to an unborn baby. (medicatione.com)
Found2
  • We found that Ponatinib, an FDA-approved drug, is an effective inhibitor of BRAF monomers and dimers. (nature.com)
  • The drug content uniformity was in between 97.90 to 99.90 %, water absorption ration were found between 51 to 80% and wetting time between 13 to 61 sec. (iajpr.com)