title: Phosphodiesterase 4 inhibitors as airways smooth muscle relaxant agents: synthesis and biological activities of triazine derivatives.
abstract: A series of triazine derivatives was synthesized. The compounds were evaluated for tracheal smooth muscle relaxant and type 4 phosphodiesterase inhibitory activities. A highly significant correlation was observed between the two effects. Two compounds exhibited potent relaxant activity (EC50: 17 and 24 nM) and might be useful for the treatment of asthma.
authors.affiliation: Institut de Chimie Pharmaceutique, Lille, France.
authors.forename: F
authors.initials: F
authors.lastname: Leroux
authors.forename: B J
authors.initials: BJ
authors.lastname: van Keulen
authors.forename: J
authors.initials: J
authors.lastname: Daliers
authors.forename: N
authors.initials: N
authors.lastname: Pommery
authors.forename: J P
authors.initials: JP
authors.lastname: Hénichart
mesh_terms: D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D009126:Muscle Relaxation / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000502:physiology; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D051381:Rats; D014132:Trachea / Q000187:drug effects* / Q000502:physiology; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D010726:Phosphodiesterase Inhibitors; D014227:Triazines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4