Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding.
The synthesis and biological properties of a series of nicotinamide ethers are described. These compounds, structurally novel calcium-independent phosphodiesterase inhibitors, also inhibit the binding of [3H]rolipram to rat brain membranes and reverse reserpine-induced hypothermia in the mouse. Several compounds exhibited potent in vivo activity comparable to the standard agent, rolipram.
Vinick
F J
FJ
Pfizer Central Research, Groton, Connecticut 06340.
Saccomano
N A
NA
Koe
B K
BK
Nielsen
J A
JA
Williams
I H
IH
Thadeio
P F
PF
Jung
S
S
Meltz
M
M
Johnson
J
J
Lebel
L A
LA
D000818:Animals; D001665:Binding Sites; D001833:Body Temperature Regulation / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D004987:Ethers; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051379:Mice; D015394:Molecular Structure; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis*; D011485:Protein Binding; D011760:Pyrrolidinones / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D012110:Reserpine / Q000494:pharmacology; D020889:Rolipram; D013329:Structure-Activity Relationship
D004987:Ethers; D007202:Indicators and Reagents; D010726:Phosphodiesterase Inhibitors; D011760:Pyrrolidinones; D009536:Niacinamide; D012110:Reserpine; D020889:Rolipram