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Synthesis of amino acid derived seven-membered lactams by RCM and their evaluation against HIV protease.

Abstract：

:A versatile synthesis of hydroxylated and epoxy 1-azepin 2-ones substituted at N1, C-3 and C-4 or C-7 has been developed. The sequence involves ring-closing metathesis of an amino acid derived diene amide, followed by either epoxidation or dihydroxylation, of the resulting alkene. Assay of the product epoxides (10, 18, 25) and diols (9a, 17, 24) against HIV protease reveals micromolar inhibition.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Zaman S,Campaner P,Abell AD

doi

10.1016/j.bmc.2006.09.009

subject

Has Abstract

pub_date

2006-12-15 00:00:00

pages

8323-31

issue

24

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(06)00725-5

journal_volume

14

pub_type

杂志文章

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