Search results for "piperidine"

showing 10 items of 236 documents

1,1′-(Diphosphene-1,2-diyl)bis(2,2,6,6-tetramethylpiperidine)

2017

The title compound, C18H36N2P2, crystallizes in the triclinic space groupP-1 with two independent molecules in the asymmetric unit. Both molecules adopt atransconfiguration of the tetramethylpiperidine units along the P=P axis. The crystal packing is stabilized only by van der Waals interactions.

crystal structurebiologyChemistryStereochemistryDiphospheneCrystal structureTriclinic crystal system010402 general chemistry010403 inorganic & nuclear chemistrybiology.organism_classification01 natural sciencesMedicinal chemistry0104 chemical scienceslow-coordinate trivalent phosphorusCrystalchemistry.chemical_compoundsymbols.namesakeTrans configurationsymbolslcsh:QD901-999TetradiphosphenePiperidinelcsh:Crystallographyvan der Waals forceIUCrData
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1,1′-[(2,3,5,6-Tetramethyl-1,4-phenylene)bis(methylene)]dipiperidine

2018

The asymmetric unit of the title compound, C22H36N2, comprises one half-molecule, the other half being generated by a center of inversion. The piperidine ring adopts a chair conformation, with the exocyclic N—C bond in an equatorial orientation. A short intramolecular C—H...N hydrogen bond occurs and forms an S(6) motif. No directional interactions beyond van der Waals contacts are observed between the molecules, which form a wave-like supramolecular architecture.

crystal structurebiologyHydrogen bondpiperidine-substituted dureneCyclohexane conformationCrystal structure010402 general chemistry010403 inorganic & nuclear chemistrybiology.organism_classificationRing (chemistry)01 natural sciencesMedicinal chemistry0104 chemical sciencesintramolecular C—H...N hydrogen bondsymbols.namesakechemistry.chemical_compoundchemistrysymbolslcsh:QD901-999TetraPiperidinelcsh:Crystallographyvan der Waals forceEne reactionIUCrData
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Organocatalytic Alcohol Oxidation Catalyzed by Recyclable TEMPO-functionalized [60]fullerene

2014

fullerene alcohol oxidation 2266-Tetramethylpiperidine 1-oxyl (TEMPO)
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C60-TEMPO-IL hybrid: “release and catch” organocatalyst for the oxidation of alcohols

2014

fullerene ionic liquids alcohol oxidation 2266-tetramethylpiperidine 1-oxyl
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CCDC 1873575: Experimental Crystal Structure Determination

2019

Related Article: Angeliki A. Athanasopoulou, Luca M. Carrella, Eva Rentschler|2019|Dalton Trans.|48|4779|doi:10.1039/C9DT00552H

hexakis(piperidin-1-ium) bis(tris(mu-2-oxidobenzene-1-carbohydroximato)-hexakis(mu-N2-dioxidobenzene-1-carboximidato)-hexa-iron-terbium) tris(piperidine) tritriacontahydrateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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Prediction of properties of chiral compounds by molecular topology

1998

Abstract A common assumption in chemistry is that chiral behavior is associated with 3-D geometry. However, chiral information is related to symmetry, which allows the topological handling of chiral atoms by weighted graphs and the calculation of new descriptors that give a weight to the corresponding entry in the main diagonal of the topological matrix. In this study, it is demonstrated that, operating in this way, chiral topological indices are obtained that can differentiate the pharmacological activity between pairs of enantiomers. The 50% inhibitory concentration (IC50) values of the D2 dopamine receptor and the σ receptor for a group of 3-hydroxy phenyl piperidines are specifically pr…

inorganic chemicalsStereochemistryIn Vitro TechniquesMain diagonalStructure-Activity RelationshipMatrix (mathematics)PiperidinesComputational chemistryMaterials ChemistryAnimalsHypnotics and SedativesReceptors sigmaheterocyclic compoundsPhysical and Theoretical ChemistrySpectroscopyGroup (mathematics)Chemistryorganic chemicalsStereoisomerismComputer Graphics and Computer-Aided DesignDopamine D2 Receptor AntagonistsCharacter (mathematics)Models ChemicalDrug DesignCentral Nervous System StimulantsMolecular topologyEnantiomerSymmetry (geometry)Chirality (chemistry)Journal of Molecular Graphics and Modelling
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Blocking Jak/STAT signalling using tofacitinib inhibits angiogenesis in experimental arthritis

2021

Abstract Objective During rheumatoid arthritis (RA), the angiogenic processes, occurring with pannus-formation, may be a therapeutic target. JAK/STAT-pathway may play a role and the aim of this work was to investigate the inhibiting role of a JAK-inhibitor, tofacitinib, on the angiogenic mechanisms occurring during RA. Methods After ethical approval, JAK-1, JAK-3, STAT-1, STAT-3 and VEGF expression was evaluated on RA-synovial-tissues. In vitro, endothelial cells (ECs), stimulated with 20 ng/ml of VEGF and/or 1 μM of tofacitinib, were assessed for tube formation, migration and proliferation, by Matrigel, Boyden chamber assay and ki67 gene-expression. In vivo, 32 mice received collagen (coll…

medicine.medical_specialtyAngiogenesisArthritisDiseases of the musculoskeletal systemPharmacologyPyrroleMiceRheumatoid arthritis Angiogenesis TofacitinibPiperidinePiperidinesIn vivoInternal medicineMedicineAnimalsHumansPyrrolesRheumatoid arthritisRheumatoid arthritiTube formationMatrigelEndothelial CellTofacitinibbusiness.industryAnimalSynovial MembraneEndothelial Cellsmedicine.diseaseArthritis ExperimentalRheumatologyAngiogenesiPyrimidinesPyrimidineRC925-935TofacitinibRheumatoid arthritisAngiogenesisbusinessHumanResearch Article
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Mucosa-dependent muscarinic liberation of prostaglandins from rat isolated trachea.

1995

1. The present study examined whether cholinoceptor stimulation modulates the release of arachidonic acid-derived mediators from rat isolate tracheae. 2. Tracheae were preincubated with [3H]-arachidonic acid and the outflow of 3H-compounds was determined. Acetylcholine and the muscarinic agonist, carbachol but not nicotine, increased the rate of tritium outflow maximally by about 30%. The M3 receptor-preferring antagonist rho-fluoro-hexahydrosiladiphenidol was more effective than pirenzepine and methoctramine in antagonizing the effect of acetylcholine. 3. High performance liquid chromatography analysis (methanol gradient) of the released 3H-compounds showed that one peak, co-eluting with […

medicine.medical_specialtyCarbacholAcetonitrilesMuscarinic AntagonistsIn Vitro TechniquesMuscarinic AgonistsMuscarinic agonistRats Sprague-Dawleychemistry.chemical_compoundPiperidinesInternal medicineMuscarinic acetylcholine receptormedicineMethoctramineAnimalsDrug InteractionsAcetylcholine receptorPharmacologyArachidonic AcidDose-Response Relationship DrugMuscarinic acetylcholine receptor M1PirenzepineAcetylcholineRatsTracheaEndocrinologychemistryProstaglandinslipids (amino acids peptides and proteins)FemaleAcetylcholinemedicine.drugResearch Article
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Different muscarine receptors mediate the prejunctional inhibition of [3H]-noradrenaline release in rat or guinea-pig iris and the contraction of the…

1989

To investigate the muscarine receptor type mediating inhibition of [3H]-noradrenaline release from the isolated rat and guinea-pig iris we have determined the potency of antimuscarinic drugs to antagonize the methacholine-induced inhibition of [3H]-noradrenaline overflow evoked by field stimulation (3 Hz, 2 min). The prejunctional apparent affinities were compared with those obtained for postjunctional muscarine receptors mediating the methacholine-induced contraction of the isolated rabbit iris sphincter muscle. Prejunctional apparent affinity constants of pirenzepine (6.67), himbacine (8.51), methoctramine (7.92), 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP, 8.00), hexahydro-d…

medicine.medical_specialtyContraction (grammar)Iris sphincter muscleIrisIn Vitro TechniquesBiologyGuinea pigNorepinephrinechemistry.chemical_compoundPiperidinesInternal medicineMuscarinic acetylcholine receptormedicineAnimalsMethacholine CompoundsNeurotransmitterReceptorPharmacologyMuscarineMuscle SmoothRats Inbred StrainsGeneral MedicineReceptors MuscarinicElectric StimulationRatsKineticsmedicine.anatomical_structureEndocrinologychemistrySphincterRabbitsMuscle ContractionNaunyn-Schmiedebergs Archives of Pharmacology
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Diacylglycerol kinase α mediatses 17-β-estradiol-induced proliferation, motility, and anchorage-independent growth of Hec-1A endometrial cancer cell …

2011

Increased levels of endogenous and/or exogenous estrogens are one of the well known risk factors of endometrial cancer. Diacylglycerol kinases (DGKs) are a family of enzymes which phosphorylate diacylglycerol (DAG) to produce phosphatidic acid (PA), thus turning off and on DAG-mediated and PA-mediated signaling pathways, respectively. DGK α activity is stimulated by growth factors and oncogenes and is required for chemotactic, proliferative, and angiogenic signaling in vitro. Herein, using either specific siRNAs or the pharmacological inhibitor R59949, we demonstrate that DGK α activity is required for 17-β-estradiol (E2)-induced proliferation, motility, and anchorage-independent growth of …

medicine.medical_specialtyGPR30medicine.drug_classCell SurvivalDiacylglycerol kinaseMotilityEstrogen receptorEnzyme AssayEndometrial carcinomaBiologyQuinazolinoneReceptors G-Protein-CoupledPiperidinePiperidinesCell MovementInternal medicineCell Line TumormedicineCell AdhesionHumansEndometrial NeoplasmEnzyme AssaysQuinazolinonesDiacylglycerol kinaseCell ProliferationEstradiolCell growthKinaseCell BiologyDiacylglycerol kinase; Endometrial carcinoma; Estrogen; GPR30; Cell BiologyEstrogenEndometrial NeoplasmsCell biologyEnzyme ActivationLipoprotein LipaseEndocrinologyReceptors EstrogenEstrogenGene Knockdown TechniquesGene Knockdown TechniqueFemaleRNA InterferenceSignal transductionGPERHuman
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