Il. Pinto et al., THE SELECTIVE-INHIBITION OF PHOSPHODIESTERASE-IV BY BENZOPYRAN DERIVATIVES OF ROLIPRAM, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1743-1746
A series of benzopyran derivatives of rolipram has been prepared, one
of which, 8a, proved to be a potent inhibitor of the PDE IV isoenzyme.
The enantiomers of 8a were separated and activity shown to reside mai
nly in the (+) enantiomer. These novel compounds display much reduced
activity on the high affinity form of PDE IV relative to rolipram.