6533b7d0fe1ef96bd1259bac
RESEARCH PRODUCT
Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system
Y. HarrakGiuseppe DaidoneMaria Dolors PujolGloria RosellDomenico SchillaciSalvatore Plesciasubject
MaleStereochemistrymedicine.drug_classClinical BiochemistryAnti-Inflammatory Agents14-benzodioxinePharmaceutical ScienceBiochemistryChemical synthesisAnti-inflammatorypyrrole nucleuRats Sprague-DawleyStructure-Activity Relationshipchemistry.chemical_compoundIn vivoDrug DiscoverymedicineAnimalsEdemaCyclooxygenase InhibitorsPyrrolesMolecular Biologyanti-inflammatoryPyrroleMolecular StructureOrganic ChemistryBenzeneBiological activityOxyquinolineIn vitroRatsCarrageenanchemistryCyclooxygenase 2Cyclooxygenase 1Molecular Medicine14-Benzodioxinedescription
A series of substituted derivatives containing the 1,4-benzodioxine or pyrrole nucleus are described. All the newly synthesized compounds were examined for their in vitro and in vivo anti-inflammatory activity. Several derivatives, including (S)-2, 14 and 17, showed more anti-inflammatory activity in vivo in these assays (rat paw oedema induced by carrageenan) than the known classical anti-inflammatory agent ibuprofen, whereas other compounds like 1 were equipotent to ibuprofen. Compound 17 was the most outstanding derivative because of its remarkable in vivo anti-inflammatory activity. In this paper, we examine and discuss the structure-activity relationships and anti-inflammatory activities of these compounds.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2007-07-01 | Bioorganic & Medicinal Chemistry |