title: Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding.
abstract: 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.
authors.affiliation: Pfizer Central Research, Groton, Connecticut 06340.
authors.forename: F J
authors.initials: FJ
authors.lastname: Vinick
authors.forename: N A
authors.initials: NA
authors.lastname: Saccomano
authors.forename: B K
authors.initials: BK
authors.lastname: Koe
authors.forename: J A
authors.initials: JA
authors.lastname: Nielsen
authors.forename: I H
authors.initials: IH
authors.lastname: Williams
authors.forename: P F
authors.initials: PF
authors.lastname: Thadeio
authors.forename: S
authors.initials: S
authors.lastname: Jung
authors.forename: M
authors.initials: M
authors.lastname: Meltz
authors.forename: J
authors.initials: J
authors.lastname: Johnson
authors.forename: L A
authors.initials: LA
authors.lastname: Lebel
mesh_terms: 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
chemical_list: D004987:Ethers; D007202:Indicators and Reagents; D010726:Phosphodiesterase Inhibitors; D011760:Pyrrolidinones; D009536:Niacinamide; D012110:Reserpine; D020889:Rolipram