Aryl sulfonamides as selective PDE4 inhibitors.
A series of novel selective phosphodiesterase 4 (PDE4) inhibitors has been developed which displays activity both in vitro and in vivo. These compounds possess good selectivity for the catalytic site of PDE4 over the high affinity Rolipram binding site. In vivo studies demonstrate a reduced propensity to display the emetic side effects which are commonly observed with PDE4 inhibitors.
Montana
J G
JG
Chiroscience Ltd, Cambridge, UK. johnmontana@chiroscience.com
Buckley
G M
GM
Cooper
N
N
Dyke
H J
HJ
Gowers
L
L
Gregory
J P
JP
Hellewell
P G
PG
Kendall
H J
HJ
Lowe
C
C
Maxey
R
R
Miotla
J
J
Naylor
R J
RJ
Runcie
K A
KA
Tuladhar
B
B
Warneck
J B
JB
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000818:Animals; D018927:Anti-Asthmatic Agents / Q000009:adverse effects / Q000138:chemical synthesis / Q000494:pharmacology; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D004802:Eosinophilia / Q000188:drug therapy; D006168:Guinea Pigs; D010726:Phosphodiesterase Inhibitors / Q000009:adverse effects / Q000138:chemical synthesis* / Q000494:pharmacology*; D011760:Pyrrolidinones / Q000009:adverse effects / Q000494:pharmacology; D020889:Rolipram; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*
D018927:Anti-Asthmatic Agents; D010726:Phosphodiesterase Inhibitors; D011760:Pyrrolidinones; D013449:Sulfonamides; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D020889:Rolipram