251306-14-6Relevant articles and documents
Synthesis of isoquino[1,2-a][2]benzazepines and biochemical testing of isomeric homoberbines and related papaverine-derivatives on the inhibition of phosphodiesterases
Meise,Onusseit,Clemens
, p. 658 - 666 (2007/10/03)
A synthesis of hitherto not accessable isoquino[1,2-a][2]benzazepines from benzoanellated seven-membered ring lactones or ε-hydroxyesters is reported; their conformation is presented. The tests of these and various similar compounds of inhibition of phosphodiesterases showed that the sterical position of one to the other benzene-ring is important. The homoberbines possess, because of their great deflexion, a weak, the norpapaverines a rather good inhibition activity: (e.g. 7, PDE III: IC50 = 1.7 μM; 8, PDE I: IC50 = 1.5 μM). For the 4,5-dihydro-3 H-2-benzazepines 13 (IC50 = 3 μM) and 14 (IC50 = 2 μM) a certain PDE IV-specifity is achieved.