Search results for "Haloketone"

showing 3 items of 3 documents

The synthesis and effect of fluorinated chalcone derivatives on nitric oxide production

2002

Abstract Dimethoxy- and trimethoxychalcone derivatives, with various patterns of fluorination, were synthesized and evaluated for their influence on nitric oxide production. Some of them, chalcones 1 , 5 , 7 , 10 , 11 and 17 , inhibited NO production with an IC 50 in the submicromolar range; 17 is especially noteworthy because of its potency (IC 50 30 nM). These effects were not the consequence of a direct inhibitory action on enzyme activity but the inhibition of enzyme expression.

LipopolysaccharidesChalconeHydrocarbons FluorinatedClinical BiochemistryNitric Oxide Synthase Type IIPharmaceutical ScienceEtherNitric OxideBiochemistryChemical synthesisCell LineNitric oxideInhibitory Concentration 50MiceStructure-Activity Relationshipchemistry.chemical_compoundChalconeDrug DiscoveryAnimalsOrganic chemistryMolecular BiologyNitriteschemistry.chemical_classificationbiologyChemistryMacrophagesAnti-Inflammatory Agents Non-SteroidalOrganic ChemistryHaloketoneCombinatorial chemistryEnzyme assayEnzymeEnzyme Inductionbiology.proteinMolecular MedicineNitric Oxide SynthaseEnoneBioorganic & Medicinal Chemistry Letters
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Entzündungshemmende wirkstoffe. XI. Ringschlußreaktion an 5-phenyl-2-thiobiuret

1988

Die Umsetzung von 5-Phenyl-2-thiobiuret (1) mil α-Chlorcarbonylverbindungen 2 fuhrt zu den N-Phenyl-N′-(2-thiazolyl)harnstoffen (3). Unter den neuen Verbindungen finden sich besonders die entzundungshemmende, anthelminthische und trichomonazide Wirksamkeit stark ausgepragt. The reaction of 5-phenyl-2-thiobiuret (1) with α-chlorocarbonyl compounds 2 leads to the structure type of N-phenyl-N1-(thiazolyl)urea (3). The new compounds exhibit particularly antiinflammatory, anthelminthic, and trichomonacidal activity.

chemistry.chemical_classificationchemistry.chemical_compoundAntiprotozoal AgentchemistryOrganic ChemistryUreaOrganic chemistryBiological activityStructure typeCondensation reactionHaloketoneJournal of Heterocyclic Chemistry
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Oxidative halogenation of substituted pyrroles with Cu(II). PartIV.Bromination of 2-(2′-hydroxybenzoyl)pyrrole. A new synthesis of bioactive analogs …

1994

The selective bromination with copper(II) bromide of the pyrrole ring in 2-(2'-hydroxybenzoyl)pyrrole (II) in the heterogeneous phase is des- cribed giving in almost quantitative yield the 4,5-dibromo derivative (VI). The subsequent introduction of halogen into the phenol moiety was observed when the reaction was perfomed in the homogeneous phase with an excess of halogenating agent. The pentabromo derivative (IX), a com- pound very active against Staphylococcus aureus (mic=17 nmoles per dm -3 ), was obtained by exhaustive bromination of the title compound. Poor yields of chloro derivatives of (II) were obtained by reaction of the parent compound with copper(II) chloride

chemistry.chemical_classificationchemistry.chemical_compoundchemistryBromideOrganic ChemistryRegioselectivityPhenolMoietyHalogenationMedicinal chemistryHaloketoneAntibacterial agentPyrroleJournal of Heterocyclic Chemistry
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