Search results for "ZOL"

showing 10 items of 4792 documents

ChemInform Abstract: Carbazole Synthesis via an in situ Trapping Strategy with Indolyl Enol Ethers.

2010

Indolyl enol ethers, generated from the alkoxy(indolyl)carbenium tetra- fluoroborates (1) by treatment with sodium hydride, can be trapped with dimethyl acetylenedicarboxylate or N-phenylmaleimide to furnish the se- lectively functionalized carbazoles (3), (4), (5), (9), (10), and (13). In addition, the biaryl derivatives (6) and (11) are produced by a ring- opening reaction of the primarily formed Diels-Alder adduct. In the case of the biaryl derivative (6), an X-ray crystal structure analysis yields valuable information on constitutions and configurations in the biaryl series. The phenomenon of atropisomerism is discussed for this compound

Dimethyl acetylenedicarboxylatechemistry.chemical_compoundAtropisomerChemistryCarbazoleAlkoxy groupGeneral MedicineRing (chemistry)EnolMedicinal chemistryAdductSodium hydrideChemInform
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ChemInform Abstract: Reaction of 2,2′-Bis(N-methylindolyl) with Dimethyl Acetylenedicarboxylate and Thermally and Photochemically Induced Cyclization…

2010

2,2′-Bis(N-methylindolyl) 1 reacts with dimethyl acetylenedicarboxylate to furnish the 3-dimethyl maleoyl-substituted 2,2′-bisindolyl 2. Compound 2 cyclizes under aluminum trichloride catalysis according to a polar process to give a cyclopenta[2,1-b:3,4-b′]diindole derivative 4. Reaction of compound 4 with benzyl-amine yields the spiro derivative 5. Photochemically-induced 1,6-electrocyclization of compound 2 gives rise to the indolo[2,3-a]carbazole 6 directly, which is readily transformed to the pyrrolo-annelated carbazole 7 by treatment with benzylamine.

Dimethyl acetylenedicarboxylatechemistry.chemical_compoundBenzylaminechemistryCarbazoleAluminum trichlorideGeneral MedicineMedicinal chemistryDerivative (chemistry)CatalysisChemInform
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Reaction of 2,2′-bis(N-methylindolyl) with dimethyl acetylenedicarboxylate and thermally- and photochemically-induced cyclizations of the product

1995

2,2′-Bis(N-methylindolyl) 1 reacts with dimethyl acetylenedicarboxylate to furnish the 3-dimethyl maleoyl-substituted 2,2′-bisindolyl 2. Compound 2 cyclizes under aluminum trichloride catalysis according to a polar process to give a cyclopenta[2,1-b:3,4-b′]diindole derivative 4. Reaction of compound 4 with benzyl-amine yields the spiro derivative 5. Photochemically-induced 1,6-electrocyclization of compound 2 gives rise to the indolo[2,3-a]carbazole 6 directly, which is readily transformed to the pyrrolo-annelated carbazole 7 by treatment with benzylamine.

Dimethyl acetylenedicarboxylatechemistry.chemical_compoundBenzylaminechemistryCarbazoleAluminum trichlorideOrganic ChemistryOrganic chemistryMedicinal chemistryDerivative (chemistry)CatalysisJournal of Heterocyclic Chemistry
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The reaction betweentriazolobenzopyridinium and triazolothiazolium ylides with dimethyl acetylenedicarboxylate

1998

Abstract The reaction of some [1,2,3]triazolo[1,5- a ]quinolinium 1,2 , [1,2,3]triazolo[5,1- a ]isoquinolinium 3,4 and [1,2,3]triazolo[5,1- b ]thiazolium 5,6 ylides with dimethyl acetylenedicarboxylate is described. Compounds as dimethyl pyrrolo[1,2- a ]quinoline-1,2-dicarboxylate 19 , dimethyl pyrrolo[2,1- a ]isoquinoline-2,3-dicarboxylate 20 , 1,1-dicyano-2,3-dimethoxycarbonyl-1 H -pyrido[1,2- a ]quinoline 24 , 4,4-dicyano-2,3-dimethoxycarbonyl-4 H -pyrido[2,1- a ]isoquinoline 25 , and 7-methyl-5,6-dimethoxy-carbonylpyrrolo[2,1- a ]thiazole 14b , are formed.

Dimethyl acetylenedicarboxylatechemistry.chemical_compoundChemistryOrganic ChemistryDrug DiscoveryQuinolineIsoquinolineThiazoleBiochemistryMedicinal chemistryTetrahedron
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Study of Reactivity in the 1,3-Dipolar Cycloaddition Reactions Leading to New Triazolopyrrolopyrazine Ring Systems

2010

The influence of the structural symmetry of the 2-pi double-reactive-sites component in the 1,3-dipolar cycloaddition reactions, involving nitrilimines as dipoles, was investigated. the experimental data showed that the loss of the symmetry leads to the formation of the monocycloadduct in good yields.

Dipole13-Dipolar Cycloaddition Reactions Triazolopyrrolopyrazine Ring SystemsChemistryOrganic Chemistry13-Dipolar cycloadditionStructural symmetryReactivity (chemistry)Ring (chemistry)PhotochemistrySettore CHIM/08 - Chimica FarmaceuticaSymmetry (physics)CycloadditionSynlett
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Peroxisome proliferator-activated receptor γ ligands regulate neural stem cell proliferation and differentiation in vitro and in vivo.

2011

Peroxisome proliferator-activated receptor gamma (PPARγ) belongs to a family of ligand-activated nuclear receptors and its ligands are known to control many physiological and pathological situations. Its role in the central nervous system has been under intense analysis during the last years. Here we show a novel function for PPARγ in controlling stem cell expansion in the adult mammalian brain. Adult rats treated with pioglitazone, a specific ligand of PPARγ, had elevated numbers of proliferating progenitor cells in the subventricular zone and the rostral migratory stream. Electron microscopy analysis also showed important changes in the subventricular zone ultrastructure of pioglitazone-t…

Doublecortin Domain ProteinsMalemedicine.medical_specialtyCell SurvivalPeroxisome proliferator-activated receptorNeural Cell Adhesion Molecule L1BiologyCerebral VentriclesRosiglitazoneCellular and Molecular NeuroscienceMicroscopy Electron TransmissionNeural Stem CellsCell MovementInternal medicineNeurosphereGlial Fibrillary Acidic ProteinmedicineAnimalsProgenitor cellRats WistarReceptorCells CulturedCell Proliferationchemistry.chemical_classificationPioglitazoneCaspase 3NeurogenesisNeuropeptidesCell DifferentiationOlfactory BulbNeural stem cellCell biologyRatsPPAR gammaAdult Stem CellsEndocrinologyNeurologychemistryNuclear receptorBromodeoxyuridineSialic AcidsThiazolidinedionesStem cell2'3'-Cyclic-Nucleotide PhosphodiesterasesMicrotubule-Associated ProteinsGlia
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Emergence of Aspergillus fumigatus azole resistance in azole-naïve patients with chronic obstructive pulmonary disease and their homes.

2017

Azole-resistant Aspergillus fumigatus (ARAF) has been reported in patients with chronic obstructive pulmonary disease (COPD) but has not been specifically assessed so far. Here, we evaluated ARAF prevalence in azole-naïve COPD patients and their homes, and assessed whether CYP51A mutations were similar in clinical and environmental reservoirs. Sixty respiratory samples from 41 COPD patients with acute exacerbation and environmental samples from 36 of these patient's homes were prospectively collected. A. fumigatus was detected in respiratory samples from 11 of 41 patients (27%) and in 15 of 36 domiciles (42%). Cyp51A sequencing and selection on itraconazole medium of clinical (n = 68) and e…

Drug Resistance Fungal -- genetics0301 basic medicineAzolesMaleAntifungal AgentsExacerbationMESH: Fungal Proteins/isolation & purification[SDV]Life Sciences [q-bio]Colony Count MicrobialAspergillus fumigatusMESH: Aspergillus fumigatus/drug effectsMESH: Cytochrome P-450 Enzyme System/drug effectsMESH: GenotypePulmonary Disease Chronic ObstructivedwellingCytochrome P-450 Enzyme SystemGenotypePulmonary Disease Chronic Obstructive -- microbiologyPrevalenceProspective Studieschemistry.chemical_classificationMESH: AgedCOPDAzole-resistanceMESH: Middle AgedbiologyMESH: Drug Resistance Fungal/geneticsMold environmental exposureSciences bio-médicales et agricolesMiddle Aged3. Good healthMESH: Pulmonary Disease Chronic Obstructive/microbiology*MESH: Housing[SDV.MP]Life Sciences [q-bio]/Microbiology and ParasitologyAir Pollution IndoorAcute DiseaseDisease ProgressionMESH: Acute DiseaseMESH: Cytochrome P-450 Enzyme System/isolation & purificationMESH: Disease ProgressionFemalemedicine.drugmedicine.medical_specialtyEnvironmental EngineeringGenotypeItraconazoleMESH: Fungal Proteins/drug effects030106 microbiologyAspergillus fumigatus -- drug effects -- genetics -- isolation & purificationMESH: Azoles/pharmacology*Fungal Proteins -- drug effects -- isolation & purificationchronic obstructive pulmonary diseaseMicrobiologyFungal Proteins03 medical and health sciencesazole resistanceMESH: Air Pollution Indoor/analysis*Drug Resistance FungalInternal medicinemedicineCOPDHumansMESH: Aspergillus fumigatus/geneticsDwellingMESH: Colony Count MicrobialMESH: PrevalenceAgedAspergillusMESH: HumansAspergillus fumigatusAzoles -- pharmacologyelectrostatic dust collectorPublic Health Environmental and Occupational Healthmold environmental exposureElectrostatic dust collectorBuilding and Constructionmedicine.diseasebiology.organism_classificationMESH: MaleMESH: Prospective StudieschemistryCytochrome P-450 Enzyme System -- drug effects -- isolation & purificationHousingAzoleARAFMESH: Aspergillus fumigatus/isolation & purification*Antifungal Agents -- pharmacologyMESH: Antifungal Agents/pharmacology*MESH: FemaleAir Pollution Indoor -- analysisIndoor air
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Uso degli inibitori di pompa protonica in un Policlinico Universitario

2012

Summary Introduction Proton pump inhibitors (PPIs) are highly prescribed drugs in Italy and in particular in the Sicilian region but little is known about their use in the hospital setting. Materials and methods PPI utilization and related costs were reviewed retrospectively by examining the pharmaceutical records of drug dispensation to the various wards of the Policlinico Universitario P. Giaccone of Palermo in 2010. Differences in the prescribing rates and drug preferences among the different clinical wards were analyzed. Results A total of 20,420 patients were hospitalized at the Policlinico of Palermo in 2010. Overall, the consumption of PPIs was 120 DDD/100 bed-days for the year 2010 …

Drug Utilizationmedicine.medical_specialtybusiness.industryHospital settingObesity SurgeryGeneral MedicinePrimary careProton pump inhibitorEsomeprazolePrescribing appropriateneSettore MED/02 - Storia Della MedicinaHospitalDrug utilizationSettore BIO/14 - FarmacologiaMedicineMedical prescriptionbusinessIntensive care medicineAdverse effectPrescribed drugsmedicine.drugDDD
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Thiazoles, Their Benzofused Systems, and Thiazolidinone Derivatives: Versatile and Promising Tools to Combat Antibiotic Resistance.

2020

Thiazoles, their benzofused systems, and thiazolidinone derivatives are widely recognized as nuclei of great value for obtaining molecules with various biological activities, including analgesic, anti-inflammatory, anti-HIV, antidiabetic, antitumor, and antimicrobial. In particular, in the past decade, many compounds bearing these heterocycles have been studied for their promising antibacterial properties due to their action on different microbial targets. Here we assess the recent development of this class of compounds to address mechanisms underlying antibiotic resistance at both bacterial-cell and community levels (biofilms). We also explore the SAR and the prospective clinical applicati…

Drug resistanceMicrobial Sensitivity Tests01 natural sciences03 medical and health scienceschemistry.chemical_compoundStructure-Activity RelationshipAntibiotic resistanceDrug DiscoveryStructure–activity relationshipAnimalsHumansThiazole030304 developmental biology0303 health sciencesThiazolidinones Antibiotic resistance BiofilmBenzeneDrug Resistance MicrobialBenzothiazoleAntimicrobialCombinatorial chemistry0104 chemical sciencesAnti-Bacterial Agents010404 medicinal & biomolecular chemistryThiazoleschemistryBiofilmsPerspectiveMolecular MedicineThiazolidinesThiazoleJournal of medicinal chemistry
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The Influence of Single-Dose and Short-Term Administration of Quercetin on the Pharmacokinetics of Midazolam in Humans.

2015

Quercetin is a plant flavonol that is available from both daily diet and nutraceuticals. To investigate the effect of acute and short-term intake of high-dose quercetin on CYP3A-mediated metabolism, 10 healthy volunteers received 7.5 mg oral midazolam without, with a single dose of 1500 mg quercetin and after 1-week supplementation with 1500 mg quercetin daily. A substudy was performed in three subjects to explore the impact of repeated quercetin intake on intravenously administered midazolam. Coadministration with a single dose of quercetin did not significantly alter the pharmacokinetics of midazolam and its 1'-hydroxymetabolite, but following short-term quercetin intake, there was a tren…

DrugAdultMalemedia_common.quotation_subjectMidazolamPharmaceutical ScienceAdministration OralPharmacologychemistry.chemical_compoundPharmacokineticsmedicineCytochrome P-450 CYP3AHumansheterocyclic compoundsDrug InteractionsAdverse effectmedia_commonCross-Over StudiesbiologyCytochrome P450MetabolismBioavailabilitychemistryArea Under Curvebiology.proteinMidazolamAdministration IntravenousFemaleQuercetinQuercetinmedicine.drugJournal of pharmaceutical sciences
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