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

Autor: Ackrell J, Antonio Y, Franco F, Landeros R, Leon A, Muchowski JM, Maddox ML, Nelson PH, Rooks WH, Roszkowski AP, Wallach MB
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1978 Oct; Vol. 21 (10), pp. 1035-44.
DOI: 10.1021/jm00208a007
Abstrakt: 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.
Databáze: MEDLINE