Substituted furans as inhibitors of the PDE4 enzyme.
The synthesis and in vitro activity of a series of substituted furans as a novel structural class of PDE4 inhibitors is described. Comparison of emetic threshold with known PDE4 inhibitors is presented.
Perrier
H
H
Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
Bayly
C
C
Laliberté
F
F
Huang
Z
Z
Rasori
R
R
Robichaud
A
A
Girard
Y
Y
Macdonald
D
D
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D005289:Ferrets; D005663:Furans / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014839:Vomiting / Q000139:chemically induced
D005663:Furans; D010726:Phosphodiesterase Inhibitors; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4