title: Aryl sulfonamides as selective PDE4 inhibitors.
abstract: 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.
authors.affiliation: Chiroscience Ltd, Cambridge, UK. johnmontana@chiroscience.com
authors.forename: J G
authors.initials: JG
authors.lastname: Montana
authors.forename: G M
authors.initials: GM
authors.lastname: Buckley
authors.forename: N
authors.initials: N
authors.lastname: Cooper
authors.forename: H J
authors.initials: HJ
authors.lastname: Dyke
authors.forename: L
authors.initials: L
authors.lastname: Gowers
authors.forename: J P
authors.initials: JP
authors.lastname: Gregory
authors.forename: P G
authors.initials: PG
authors.lastname: Hellewell
authors.forename: H J
authors.initials: HJ
authors.lastname: Kendall
authors.forename: C
authors.initials: C
authors.lastname: Lowe
authors.forename: R
authors.initials: R
authors.lastname: Maxey
authors.forename: J
authors.initials: J
authors.lastname: Miotla
authors.forename: R J
authors.initials: RJ
authors.lastname: Naylor
authors.forename: K A
authors.initials: KA
authors.lastname: Runcie
authors.forename: B
authors.initials: B
authors.lastname: Tuladhar
authors.forename: J B
authors.initials: JB
authors.lastname: Warneck
mesh_terms: 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*
chemical_list: 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