Dunn J P, Green D M, Harrison I T, Nelson P H, Pfister J R, Roszkowski A P, Untch K G
J Med Chem. 1979 Nov;22(11):1357-63. doi: 10.1021/jm00197a015.
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.
本文描述了在1、2、3或10位带有羧基基团且在7、8或9位带有各种取代基的44种5H-二苯并[a,d]环庚烯-5-酮衍生物的合成。一些化合物在豚鼠中显示出显著的支气管扩张活性，并能保护动物免受通过气雾剂或静脉注射给予的组胺攻击。活性最高的化合物是在9位带有甲基或卤素取代基的10,11-二氢-5H-二苯并[a,d]环庚烯-5-酮-2-羧酸。这些化合物通过腹腔注射给药时的活性与氨茶碱大致相当。
