8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4).
Buckley
George M
GM
Celltech R&D, Granta Park, Great Abington, Cambridge CB1 6GS, UK.
Cooper
Nicola
N
Dyke
Hazel J
HJ
Galleway
Fiona P
FP
Gowers
Lewis
L
Haughan
Alan F
AF
Kendall
Hannah J
HJ
Lowe
Christopher
C
Maxey
Robert
R
Montana
John G
JG
Naylor
Robert
R
Oxford
Janet
J
Peake
Joanna C
JC
Picken
C Louise
CL
Runcie
Karen A
KA
Sabin
Verity
V
Sharpe
Andrew
A
Warneck
Julie B H
JB
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000577:Amides / Q000494:pharmacology / Q000627:therapeutic use*; D018927:Anti-Asthmatic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D001249:Asthma / Q000188:drug therapy*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D006801:Humans; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*
D000577:Amides; D018927:Anti-Asthmatic Agents; D010726:Phosphodiesterase Inhibitors; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4