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Synthesis and evaluation of novel prodrugs of caspase inhibitors.

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Charrier JD,Durrant SJ,Studley J,Lawes L,Weber P

doi

10.1016/j.bmcl.2011.10.102

subject

Has Abstract

pub_date

2012-01-01 00:00:00

pages

485-8

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01509-5

journal_volume

22

pub_type

杂志文章

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