Phosphodiesterase 4 inhibitors as airways smooth muscle relaxant agents: synthesis and biological activities of triazine derivatives.
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.
Leroux
F
F
Institut de Chimie Pharmaceutique, Lille, France.
van Keulen
B J
BJ
Daliers
J
J
Pommery
N
N
Hénichart
J P
JP
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*
D010726:Phosphodiesterase Inhibitors; D014227:Triazines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4