Abstract
Acetic acid derivatives of tricyclic systems, such as 6,11-dihydro-11-oxodibenzo[b,e]thiepin, 4,10-dihydro-4-oxo-thieno[2,3-c][1]benzothiepin, dibenzo[b,f]thiepin, dibenz[b,f]oxepin, etc., were synthesized and assayed for antiinflammatory activity. One of the compounds, 6,11-dihydro-11-oxodibenzo[b,e]thiepin-3-acetic acid (52), was chosen for evaluation in man on the basis of high antiinflammatory activity in both short- and long-term animal assays and a low gastric irritation liability in rats and dogs.
MeSH terms
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Acetates / chemical synthesis
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Acetates / pharmacology
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Animals
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Anti-Inflammatory Agents / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Arthritis, Experimental / physiopathology
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Carrageenan
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Chemical Phenomena
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Chemistry
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Dibenzothiepins / chemical synthesis*
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Dibenzothiepins / pharmacology
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Dogs
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Edema / physiopathology
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Female
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Gossypium
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Granuloma / physiopathology
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Male
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Mice
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Quinones / antagonists & inhibitors
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Rats
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Stomach Ulcer / chemically induced
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Structure-Activity Relationship
Substances
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Acetates
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Anti-Inflammatory Agents
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Anti-Inflammatory Agents, Non-Steroidal
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Dibenzothiepins
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Quinones
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Carrageenan