Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.
This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE IV) inhibitors. Several of the quaternary substituted lactams presented possess low nanomolar IC50's for PDE IV inhibition.
Hulme
C
C
Rhône-Poulenc Rorer Central Research, Collegeville, PA 19426, USA.
Moriarty
K
K
Huang
F C
FC
Mason
J
J
McGarry
D
D
Labaudiniere
R
R
Souness
J
J
Djuric
S
S
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D007769:Lactams / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D007769:Lactams; D010726:Phosphodiesterase Inhibitors; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4