Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents / chemistry
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Anti-Inflammatory Agents / pharmacology*
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Anti-Inflammatory Agents / therapeutic use
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Benzene / chemistry*
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Cyclooxygenase 1 / metabolism
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Cyclooxygenase 2 / metabolism
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Cyclooxygenase Inhibitors / chemical synthesis
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Edema / drug therapy
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Edema / pathology
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Male
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Molecular Structure
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Oxyquinoline / chemical synthesis
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Oxyquinoline / chemistry*
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Oxyquinoline / pharmacology*
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Oxyquinoline / therapeutic use
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Pyrroles / chemical synthesis*
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Pyrroles / chemistry
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Pyrroles / pharmacology*
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Pyrroles / therapeutic use
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents
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Cyclooxygenase Inhibitors
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Pyrroles
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Oxyquinoline
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Cyclooxygenase 1
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Cyclooxygenase 2
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Benzene