Search results for "ZOL"

showing 10 items of 4792 documents

Modular synthesis of tetrasubstituted imidazoles and trisubstituted oxazoles by aldimine cross-coupling.

2008

Couplingchemistry.chemical_classificationAldimineChemistryStereochemistryOrganic ChemistryImidazolesGeneral ChemistryCrystallography X-RayCatalysisUmpolungC c couplingCyclizationIminesOxazolesCarbanionChemistry (Weinheim an der Bergstrasse, Germany)
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Hsp60 Inhibitors and Modulators

2019

In this chapter, we focus on the 60 KDa Heat Shock Protein (Hsp60) and discuss some of its biological, molecular and pathological features. The structural and mechanistic aspect of the Hsp60 folding cycle will be also presented. We further illustrate how Hsp60 may be involved in many diseases and therefore considered as an effective therapeutic or theranostic target. Finally, the state-of-the-art on the development of Hsp60 and bacterial GroEL inhibitors and modulators of their expression will be illustrated. This is discussed in the light of a negative chaperonotherapy, and the consequent development of inhibitors, as well as positive chaperonotherapy, in the event its excessive activity i…

Cpn60Excessive activityHsp60 inhibitoranimal structuresHeat shock proteinChemistryPyrazolopyrimidinefungiAvrainvillamidechemical and pharmacologic phenomenaComputational biologyMizoribineSettore CHIM/06 - Chimica OrganicaCarboranylphenoxyacetanilideHsp60complex mixturesGroELGroELHspD1Heat shock proteinHSP60AvrainvillamideEpolactaene
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Adalimumab vs Azathioprine in the Prevention of Postoperative Crohn's Disease Recurrence. A GETECCU Randomised Trial.

2017

Background and aims Postoperative recurrence of Crohn's disease [POR-CD] is almost certain if no prophylaxis is administered. Evidence for optimal treatment is lacking. Our aim was to compare the efficacy of adalimumab [ADA] and azathioprine [AZA] in this setting. Methods We performed a phase 3, 52-week, multicentre, randomised, superiority study [APPRECIA], in which patients with ileocolonic resection were randomised either to ADA 160-80-40 mg subcutaneously [SC] or AZA 2.5 mg/kg/day, both associated with metronidazole. The primary endpoint was endoscopic recurrence at 1 year [Rutgeerts i2b, i3, i4], as evaluated by a blinded central reader. Results We recruited 91 patients [median age 35.…

Crohn’s diseaseAdultMalemedicine.medical_specialtyAzathioprineGastroenterology03 medical and health sciences0302 clinical medicineCrohn DiseaseInternal medicineadalimumabAzathioprinemedicineClinical endpointAdalimumabSecondary PreventionHumansAdverse effectPostoperative CareCrohn's diseaseazathioprinebusiness.industryAdalimumabGastroenterologyGeneral Medicinemedicine.diseaseSurgeryDiscontinuationCrohn's diseaseMetronidazole030220 oncology & carcinogenesisUnselected population030211 gastroenterology & hepatologyFemalebusinessImmunosuppressive Agentsmedicine.drug
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Effects of SCA40 on human isolated bronchus and human polymorphonuclear leukocytes: comparison with rolipram, SKF94120 and levcromakalim

1996

1. SCA40 (0.1 nM-0.1 mM) produced concentration-dependent suppression of the spontaneous tone of human isolated bronchus (-log EC50 = 6.85 +/- 0.09; n = 10) and reached a maximal relaxation similar to that of theophylline (3 mM). The potency (-log EC50 values) of SCA40 compared to other relaxants was rolipram (7.44 +/- 0.12; n = 9) > SCA40 > or = levcromakalim (6.49 +/- 0.04; n = 6) > SKF94120 (5.87 +/- 0.10; n = 9). 2. When tested against the activity of the isoenzymes of cyclic nucleotide phosphodiesterase (PDE) isolated from human bronchus, SCA40 proved highly potent against PDE III (-log IC50 = 6.47 +/- 0.16; n = 4). It was markedly less potent against PDE IV (4.82 +/- 0.18; n = 4) and …

Cromakalimmedicine.medical_specialtyCardiotonic AgentsNeutrophilsLeukotriene B4Muscle Relaxationchemistry.chemical_elementBronchiIn Vitro TechniquesCalciumPharmacologyLeukotriene B4chemistry.chemical_compound3'5'-Cyclic-GMP PhosphodiesterasesSuperoxidesInternal medicinemedicineHumansBenzopyransPyrrolesRolipramCyclic Nucleotide Phosphodiesterases Type 5PharmacologyCyclic nucleotide phosphodiesterasePhosphoric Diester HydrolasesSuperoxideAnti-Inflammatory Agents Non-SteroidalElastaseImidazolesN-Formylmethionine leucyl-phenylalanineCyclic Nucleotide Phosphodiesterases Type 3PyrrolidinonesBronchodilator AgentsCyclic Nucleotide Phosphodiesterases Type 4N-Formylmethionine Leucyl-PhenylalanineEndocrinologychemistry3'5'-Cyclic-AMP PhosphodiesterasesPyrazinesCalciumLeukocyte ElastaseRolipramCromakalimResearch Articlemedicine.drugBritish Journal of Pharmacology
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1,1′-[2,3,5,6-Tetramethyl-p-phenylenebis(methyleneoxy)]di-1H-benzotriazole

2009

The complete molecule of the title compound, C(24)H(24)N(6)O(2), is generated by a crystallographic inversion centre. The benzotriazole rings form dihedral angles of 2.10 (7)° with the central aromatic ring. The crystal packing is consolidated by π-π inter-actions, with centroid-centroid distances of 3.6234 (10) Å, together with weak C-H⋯π inter-actions.

Crystalchemistry.chemical_compoundBenzotriazoleChemistryMoleculeGeneral Materials ScienceGeneral ChemistryDihedral angleCondensed Matter PhysicsBioinformaticsRing (chemistry)Organic PapersMedicinal chemistryActa Crystallographica Section E Structure Reports Online
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Bis[3-methyl-5-(pyridin-2-yl)-1H-pyrazol-4-yl] selenide methanol hemisolvate

2014

The asymmetric unit of the title compound, C18H16N6Se·0.5CH3OH, contains two independent molecules of bis[3-methyl-5-(pyridin-2-yl)-1H-pyrazol-4-yl] selenide with similar C—Se—C bond angles [99.30 (14) and 98.26 (13)°], and a methanol molecule of solvation. In one molecule, the dihedral angles between pyrazole and neighbouring pyridine rings are 18.3 (2) and 15.8 (2)°, and the corresponding angles in the other molecule are 13.5 (2) and 8.3 (2)°. In the crystal, the selenide and solvent molecules are linked by classical O—H...N and N—H...N hydrogen bonds, as well as by weak C—H...O and C—H...π interactions, forming a three-dimensional supramolecular architecture.

Crystallography010405 organic chemistryHydrogen bondSolvationGeneral ChemistryPyrazoleDihedral angle010402 general chemistryCondensed Matter PhysicsBioinformaticsOrganic Papers01 natural sciences3. Good health0104 chemical scienceschemistry.chemical_compoundCrystallographyMolecular geometrychemistryQD901-999SelenidePyridineMoleculeGeneral Materials ScienceActa Crystallographica Section E Structure Reports Online
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1-(2,3,5,6-Tetramethylbenzyloxy)-1H-benzotriazole

2009

In the title compound, C17H19N3O, the benzotriazole ring is essentially planar, with a maximum deviation of 0.0069 (15) Å. The mean plane of the benzotriazole ring forms a dihedral angle of 13.16 (4)° with the mean plane of the benzene ring. The crystal packing is stabilized by π–π stacking interactions, with a centroid–centroid distance of 3.8077 (12) Å, together with weak C—H...π interactions. Molecules are stacked along the a axis.

CrystallographyBenzotriazolebiologyPlane (geometry)StackingGeneral ChemistryDihedral angleCondensed Matter PhysicsBioinformaticsRing (chemistry)biology.organism_classificationOrganic PapersCrystalchemistry.chemical_compoundCrystallographychemistryQD901-999TetraGeneral Materials ScienceBenzeneActa Crystallographica Section E Structure Reports Online
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N-(5-Amino-1H-1,2,4-triazol-3-yl)pyridine-2-carboxamide

2013

The title compound, C8H8N6O, was obtained by the reaction of 3,5-diamino-1,2,4-triazole with ethyl 2-picolinate in a glass oven. The dihedral angles formed between the plane of the amide group and the pyridine and triazole rings are 11.8 (3) and 5.8 (3)°, respectively. In the crystal, an extensive system of classical N—H...N and N—H...O hydrogen bonds generate an infinite three-dimensional network.

CrystallographyChemistryHydrogen bondmedicine.drug_classTriazoleCarboxamideGeneral ChemistryDihedral angleCondensed Matter PhysicsBioinformaticsOrganic PapersMedicinal chemistryCrystalchemistry.chemical_compoundQD901-999AmidePyridinemedicineGeneral Materials ScienceActa Crystallographica Section E Structure Reports Online
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A C(π-hole)⋯Cl-Zn tetrel interaction driving a metal-organic supramolecular assembly

2020

A brominated pyrimidinyl triazolopyridine ligand (bptpy) forms a C(π-hole)⋯Cl-Zn tetrel interaction that plays a determining role in the formation of supramolecular layers through chain assembly in 18 membered metallacycle [(ZnCl2)2(μ-bptpy)2] crystals. Supramolecular chains are formed through C-H⋯X interactions. The observed interactions are supported by DFT calculations using model dimers. This journal is

CrystallographyChemistryLigandSupramolecular chemistryGeneral Materials ScienceTriazolopyridineGeneral ChemistryMetallacycleCondensed Matter PhysicsSupramolecular assemblyCrystEngComm 22: 6979-6982 (2020)
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ChemInform Abstract: Synthesis and Characterization of the Acetazolamide Complexes of Co(II) and Zn(II).

1987

Abstract The preparation and characterization of the complexes of Acetazolamide (Acm) with Co(II) and Zn(II) are described. The complexes are of the type M(Acm) 2 (NH 3 ) 2 . Monodentate or bidentate behaviour of Acm from the electronic properties and the IR spectral data is discussed. The probable structures of the complexes are proposed.

CrystallographyDenticityChemistrymedicineGeneral MedicineAcetazolamideSpectral dataElectronic propertiesmedicine.drugCharacterization (materials science)ChemInform
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