Novel 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones as IMPDH inhibitors

Helen L Birch; George M Buckley; Natasha Davies; Hazel J Dyke; Elizabeth J Frost; Philip J Gilbert; Duncan R Hannah; Alan F Haughan; Michael J Madigan; Trevor Morgan; William R Pitt; Andrew J Ratcliffe; Nicholas C Ray; Marianna D Richard; Andrew Sharpe; Alicia J Taylor; Justine M Whitworth; Sophie C Williams

doi:10.1016/j.bmcl.2005.06.108

Novel 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones as IMPDH inhibitors

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5335-9. doi: 10.1016/j.bmcl.2005.06.108. Epub 2005 Oct 3.

Authors

Helen L Birch¹, George M Buckley, Natasha Davies, Hazel J Dyke, Elizabeth J Frost, Philip J Gilbert, Duncan R Hannah, Alan F Haughan, Michael J Madigan, Trevor Morgan, William R Pitt, Andrew J Ratcliffe, Nicholas C Ray, Marianna D Richard, Andrew Sharpe, Alicia J Taylor, Justine M Whitworth, Sophie C Williams

Affiliation

¹ UCB Celltech, Granta Park, Great Abington, Cambridge, CB1 6GS, UK.

PMID: 16202581
DOI: 10.1016/j.bmcl.2005.06.108

Abstract

The synthesis and biological activity of a novel series of 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones are described. Some of these compounds were found to be potent inhibitors of inosine 5'-monophosphate dehydrogenase type II (IMPDH II).

MeSH terms

Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Humans
IMP Dehydrogenase / antagonists & inhibitors*
Molecular Conformation
Quinazolines / chemical synthesis
Quinazolines / chemistry*
Quinazolines / pharmacology*
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Quinazolines
IMP Dehydrogenase
IMPDH2 protein, human