| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10593253 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
A novel type of caspase inhibitor prodrug that improves systemic exposure after oral administration in rats has been designed. Such a prodrug, based on a 6,6a-dihydrofuro[3,2-d]oxazol-5(3aH)-one motif, has the advantage of rapidly liberating the active inhibitor without producing any cleavage by-product. Prodrugs 6-8, are synthesised in a high yielding one-step transformation from the active parents with high diastereomeric excess.
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Authors
Jean-Damien Charrier, Steven J. Durrant, John Studley, Linda Lawes, Peter Weber,