Low molecular weight indole fragments as IMPDH inhibitors

Rebekah E Beevers; George M Buckley; Natasha Davies; Joanne L Fraser; Francis C Galvin; Duncan R Hannah; Alan F Haughan; Kerry Jenkins; Stephen R Mack; William R Pitt; Andrew J Ratcliffe; Marianna D Richard; Verity Sabin; Andrew Sharpe; Sophie C Williams

doi:10.1016/j.bmcl.2006.01.089

Low molecular weight indole fragments as IMPDH inhibitors

Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. doi: 10.1016/j.bmcl.2006.01.089. Epub 2006 Feb 17.

Authors

Rebekah E Beevers¹, George M Buckley, Natasha Davies, Joanne L Fraser, Francis C Galvin, Duncan R Hannah, Alan F Haughan, Kerry Jenkins, Stephen R Mack, William R Pitt, Andrew J Ratcliffe, Marianna D Richard, Verity Sabin, Andrew Sharpe, Sophie C Williams

Affiliation

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

PMID: 16483769
DOI: 10.1016/j.bmcl.2006.01.089

Abstract

The study of non-oxazole containing indole fragments as inhibitors of inosine monophosphate dehydrogenase (IMPDH) is described. The synthesis and in vitro inhibitory values for IMPDH II are discussed.

MeSH terms

Carbamates / chemistry
Carbamates / pharmacology
Crystallography, X-Ray
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Hydrogen Bonding
IMP Dehydrogenase / antagonists & inhibitors*
Indoles / chemical synthesis
Indoles / chemistry
Indoles / pharmacology*
Models, Molecular
Molecular Structure
Molecular Weight
Oxazoles / pharmacology
Phenylurea Compounds / chemistry
Phenylurea Compounds / pharmacology
Sensitivity and Specificity
Structure-Activity Relationship

Substances

Carbamates
Enzyme Inhibitors
Indoles
N-3-(3-(3-methoxy-4-oxazol-5-ylphenyl)ureido)benzylcarbamic acid tetrahydrofuran-3-yl ester
Oxazoles
Phenylurea Compounds
IMP Dehydrogenase
BMS-337197