7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma

G Buckley; N Cooper; H J Dyke; F Galleway; L Gowers; J C Gregory; D R Hannah; A F Haughan; P G Hellewell; H J Kendall; C Lowe; R Maxey; J G Montana; R Naylor; C L Picken; K A Runcie; V Sabin; B R Tuladhar; J B Warneck

doi:10.1016/s0960-894x(00)00426-1

7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma

Bioorg Med Chem Lett. 2000 Sep 18;10(18):2137-40. doi: 10.1016/s0960-894x(00)00426-1.

Authors

Affiliation

¹ Celltech-Chiroscience Ltd, Abington, Cambridge, UK.

PMID: 10999488
DOI: 10.1016/s0960-894x(00)00426-1

Abstract

The synthesis and pharmacological profile of a novel series of 7-methoxybenzofuran-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4).

MeSH terms

3',5'-Cyclic-AMP Phosphodiesterases / antagonists & inhibitors*
Administration, Oral
Animals
Asthma / drug therapy
Benzamides / adverse effects
Benzamides / chemical synthesis
Benzamides / pharmacology
Benzofurans / adverse effects
Benzofurans / chemical synthesis*
Benzofurans / pharmacology*
Cyclic Nucleotide Phosphodiesterases, Type 4
Eosinophilia / drug therapy
Guinea Pigs
Inhibitory Concentration 50
Phosphodiesterase Inhibitors / adverse effects
Phosphodiesterase Inhibitors / chemical synthesis*
Phosphodiesterase Inhibitors / pharmacology
Pyridines / adverse effects
Pyridines / chemical synthesis
Pyridines / pharmacology
Rolipram / adverse effects
Rolipram / analogs & derivatives
Rolipram / pharmacology
Structure-Activity Relationship
Vomiting / chemically induced

Substances

Benzamides
Benzofurans
Phosphodiesterase Inhibitors
Pyridines
3',5'-Cyclic-AMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 4
Rolipram
piclamilast