Synthesis and biological evaluation of 2,5-dihydropyrazol.
A novel series of 2,5-dihydropyrazolo[4,3-c]quinolin-3-ones has been prepared. These compounds showed good PDE 4 inhibitory activity and weak affinity for rolipram's binding site. They also exhibited a good anti-inflammatory profile without emetic side effects.
Crespo
M I
MI
Almirall Prodesfarma, Research Centre, Barcelona, Spain. macrespo@almirallprodesfarma.com
Gràcia
J
J
Puig
C
C
Vega
A
A
Bou
J
J
Beleta
J
J
Doménech
T
T
Ryder
H
H
Segarra
V
V
Palacios
J M
JM
D000818:Animals; D018927:Anti-Asthmatic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004639:Emetics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008958:Models, Molecular; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D018927:Anti-Asthmatic Agents; D004639:Emetics; D010726:Phosphodiesterase Inhibitors; D015363:Quinolones