Dibenzotropone- and dibenzosuberonecarboxylic acids with bronchodilator activity.

Autor: Dunn JP, Green DM, Harrison IT, Nelson PH, Pfister JR, Roszkowski AP, Untch KG
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1979 Nov; Vol. 22 (11), pp. 1357-63.
DOI: 10.1021/jm00197a015
Abstrakt: The syntheses of 44 5H-dibenzo[a,d]cyclohepten-5-one derivatives bearing a carboxyl gropu at the 1, 2, 3, or 10 position and various substituents at the 7, 8, or 9 position are described. Some of the compounds showed significant bronchodilator activity in guinea pigs and protected the animals against a histamine challenge administered either by aerosol or intravenously. The most active compounds were 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one-2-carboxylic acids bearing a methyl or halogen substituent at the 9 position. These compounds were approximately as active as aminophylline by intraperitoneal administration.
Databáze: MEDLINE