Search results for "Indole"

showing 10 items of 570 documents

New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation.

2018

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40&ndash

0301 basic medicinethiazole derivativeAquatic OrganismsIndolesDrug ResistancePharmaceutical ScienceBacterial growthAntibiofilm agentmedicine.disease_cause01 natural scienceschemistry.chemical_compoundDrug Discoveryanti-virulence agents; antibiofilm agents; marine alkaloids; nortopsentin analogues; thiazole derivatives; Anti-Bacterial Agents; Aquatic Organisms; Biofilms; Humans; Imidazoles; Indoles; Inhibitory Concentration 50; Staphylococcal Infections; Staphylococcus aureus; Thiazoles; Drug Resistance; Bacterial; Anti-virulence agents; Antibiofilm agents; Marine alkaloids; Nortopsentin analogues; Thiazole derivativesPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Aquatic OrganismBiofilmBacterialImidazolesantibiofilm agentsStaphylococcal InfectionsAnti-Bacterial Agentsnortopsentin analoguesBiochemistryStaphylococcus aureusStaphylococcus aureumarine alkaloidsthiazole derivativesSelectivityHumanStaphylococcus aureusAnti-virulence agentNortopsentin analogueArticle03 medical and health sciencesInhibitory Concentration 50Anti-Bacterial AgentDrug Resistance BacterialIc50 valuesmedicineHumansThiazoleImidazoleStaphylococcal Infection010405 organic chemistryBiofilmSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesmarine alkaloidThiazoles030104 developmental biologychemistrylcsh:Biology (General)anti-virulence agentsIndoleBiofilmsThiazoleMarine drugs
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CCDC 289303: Experimental Crystal Structure Determination

2007

Related Article: K.Laihia, A.Valkonen, E.Kolehmainen, A.Antonov, D.Zhukov, I.Fedosov, V.Nikiforov|2006|J.Mol.Struct.|800|100|doi:10.1016/j.molstruc.2006.03.095

11'22'5'6'7'7a'-octahydro-2-oxo-1'-nitro-2'-(4''-chlorophenyl)-spiro(3H-indole-33'-(3H)-pyrrolizine)Space GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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Synthesis of Isoxazole and 1,2,3-Triazole Isoindole Derivatives via Silver- and Copper-Catalyzed 1,3-Dipolar Cycloaddition Reaction.

2016

International audience; The CuI-or Ag 2 CO 3-catalyzed [3+2] cycloaddition of propargyl-substituted dihydroisoindolin-1-one (3) with arylnitrile oxides 1a-d (Ar = Ph, p-MeC 6 H 4 , p-MeOC 6 H 4 , p-ClC 6 H 4) produces in good yields novel 3,5-disubstituted isoxazoles 4 of the ethyl-2-benzyl-3-oxo-1-((3-arylisoxazol-5yl)methyl)-2,3-dihydro-1H-isoindole-1-carboxylate type. With aryl azides 2a-d (Ar = Ph, p-MeC 6 H 4 , p-OMeC 6 H 4 , p-ClC 6 H 4), a series of 1,4-disubstituted 1,2,3-triazoles 6 (ethyl-2-benzyl-3-oxo-1-((1-aryl-1H-1,2,3-triazol-4-yl)methyl)-2,3-dihydro-1H-isoindole-1-carboxylates) was obtained. The reactions proceed in a regioselective manner affording exclusively racemic adduc…

123-TriazoleMagnetic Resonance SpectroscopySilverSpectrophotometry Infrared12Pharmaceutical Science[3+2] dipolar cycloaddition; arylnitrile oxides; arylazides; isoxazole; 123-triazolesarylazidesIsoindoles010402 general chemistryCrystallography X-Ray01 natural sciencesMedicinal chemistryCatalysisArticleAnalytical Chemistrylcsh:QD241-441chemistry.chemical_compoundlcsh:Organic chemistryDrug DiscoveryOrganic chemistryPhysical and Theoretical ChemistryIsoxazoleCycloaddition Reaction010405 organic chemistryArylOrganic ChemistryisoxazoleRegioselectivityIsoxazolesarylnitrile oxidesTriazolesCycloaddition0104 chemical scienceschemistryChemistry (miscellaneous)13-Dipolar cycloaddition[3+2] dipolar cycloadditionMolecular Medicine123-triazoles3-triazolesIsoindoleSelectivity[PHYS.ASTR]Physics [physics]/Astrophysics [astro-ph]CopperMolecules (Basel, Switzerland)
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CCDC 1889531: Experimental Crystal Structure Determination

2019

Related Article: Qiang Liu, Xiang‐Yu Chen, Sun Li, Kari Rissanen, Dieter Enders|2019|Adv.Synth.Catal.|361|1991|doi:10.1002/adsc.201900065

1-ethyl-6'H-spiro[indole-310'-pyrido[12-c][123]benzoxathiazine]-26'6'8'(1H9'H)-tetroneSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 930311: Experimental Crystal Structure Determination

2013

Related Article: Aaron Breivogel, Michael Meister, Christoph Förster, Frédéric Laquai, Katja Heinze|2013|Chem.-Eur.J.|19|13745|doi:10.1002/chem.201302231

2-(26-Dichloropyridin-4-yl)-1H-isoindole-13(2H)-dioneSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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Asymmetric synthesis of 3,3′-pyrrolidinyl-dispirooxindoles via a one-pot organocatalytic Mannich/deprotection/aza-Michael sequence

2016

Chemical communications 52, 2249-2252 (2016). doi:10.1039/C5CC10057G

3'-pyrrolidinyl-spirooxindole3010405 organic chemistryChemistryMannich/deprotection/aza-Michael sequenceMetals and AlloysEnantioselective synthesisSequence (biology)General Chemistrychemistry010402 general chemistry54001 natural sciencesCombinatorial chemistryCatalysis0104 chemical sciencesSurfaces Coatings and FilmsElectronic Optical and Magnetic MaterialsCatalysisStereocenterddc:540Materials ChemistryCeramics and CompositesStereoselectivityta116
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SYNTHESIS AND ANTITUMOR ACTIVITY OF 2,5-BIS(3'-INDOLYL)-FURANS AND 3,5-BIS(3'-INDOLIY)-ISOXAZOLES, NORTOPSENTIN ANALOGUES

2010

Abstract A series of novel 2,5-bis(3′-indolyl)furans and 3,5-bis(3′-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially 5 isoxazoles and 3 furan derivatives were tested against a panel of 10 human tumor cell lines and the most active derivatives 3c and 4a were selected to be evaluated in an extended panel of 29 cell lines. By exhibiting mean IC50 values of 17.4 μg/mL (3a) and 20.5 μg/mL (4c), in particular 4c showed a high level of tumor selectivity toward the 29 cell lines.

35-BIS(3'-INDOLIY)-ISOXAZOLESIndolesStereochemistry3Clinical Biochemistry2Pharmaceutical ScienceAntineoplastic AgentsBiochemistryChemical synthesis25-BIS(3'-INDOLYL)-FURANSchemistry.chemical_compound2; 5-BIS(3'-INDOLYL)-FURANS; 3; 5-BIS(3'-INDOLIY)-ISOXAZOLES; NORTOPSENTIN; ANTITUMOR ACTIVITYFuranCell Line TumorNeoplasmsDrug DiscoveryHumans5-BIS(3'-INDOLIY)-ISOXAZOLESCytotoxicityFurans5-BIS(3'-INDOLYL)-FURANSMolecular BiologyAntitumor activityAlkaloidOrganic ChemistryBiological activityNORTOPSENTINIsoxazolesSettore CHIM/08 - Chimica FarmaceuticaIn vitroANTITUMOR ACTIVITYchemistryCell cultureMolecular MedicineDrug Screening Assays Antitumor
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SYNTHESIS OF 3-(2-PHENYL-1,3-THIAZOL-4-YL)-1H-INDOLES, NEW DERIVATIVES WITH POTENTIAL ANTINEOPLASTIC ACTIVITY

2008

3-(2-PHENYL-13-THIAZOL-4-YL)-1H-INDOLESSettore CHIM/08 - Chimica Farmaceutica
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CCDC 788373: Experimental Crystal Structure Determination

2010

Related Article: C.Rizzoli, P.Astolfi, E.Marku, L.Greci|2010|Acta Crystallogr.,Sect.E:Struct.Rep.Online|66|o1986|doi:10.1107/S1600536810026176

3-Benzyl-3-hydroxy-2-phenyl-3H-indole 1-oxideSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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Isoxazolo[5,4-e]isoindole a new ring system with potent antitumor activity

2011

4-e]isoindoleIsoxazolo[5; 4-e]isoindole; Combretastatin; antitumor agentsCombretastatinIsoxazolo[5antitumor agentsIsoxazolo[54-e]isoindole Combretastatin antitumor agents
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