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Synthesis and antiinflammatory activity of 6,11-dihydro-11-oxodibenzo[b,e]thiepinalkanoic acids and related compounds.

作者信息

Ackrell J, Antonio Y, Franco F, Landeros R, Leon A, Muchowski J M, Maddox M L, Nelson P H, Rooks W H, Roszkowski A P, Wallach M B

出版信息

J Med Chem. 1978 Oct;21(10):1035-44. doi: 10.1021/jm00208a007.

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.

摘要

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