Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase

G C Crawley; T G Bird; P Bruneau; R I Dowell; P N Edwards; S J Foster; J M Girodeau; R M McMillan; E R Walker; D Waterson

Structure and activity relationships leading to the discovery of ICI D2138, a selective, potent and orally active inhibitor of 5-lipoxygenase

J Lipid Mediat. 1993 Mar-Apr;6(1-3):249-57.

Authors

G C Crawley¹, T G Bird, P Bruneau, R I Dowell, P N Edwards, S J Foster, J M Girodeau, R M McMillan, E R Walker, D Waterson

Affiliation

¹ Research Department 1, ICI Pharmaceuticals, Alderley Park, Macclesfield, UK.

PMID: 8395247

Abstract

Structure and activity relationships of (methoxyalkyl)thiazole and 4-methoxytetrahydropyran series of 5-lipoxygenase inhibitors are reviewed. One member of the 4-methoxytetrahydropyran series, 6-([fluoro-5-(4-methoxy-3,4,5,6-tetrahydro-2H-pyran-4-yl)phenoxy]methyl) -1- methylquinol-2-one (ICI D2138), is undergoing clinical evaluation.

Publication types

Comparative Study

MeSH terms

Administration, Oral
Animals
Humans
In Vitro Techniques
Leukotriene B4 / biosynthesis
Lipoxygenase Inhibitors*
Pyrans / administration & dosage
Pyrans / chemistry
Pyrans / pharmacology*
Quinolones / administration & dosage
Quinolones / chemistry
Quinolones / pharmacology*
Rats
Structure-Activity Relationship
Thiazoles / chemistry
Thiazoles / pharmacology

Substances

Lipoxygenase Inhibitors
Pyrans
Quinolones
Thiazoles
ICI D2138
Leukotriene B4