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https://hdl.handle.net/2440/34879
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Type: | Journal article |
Title: | Synthesis of amino acid derived seven-membered lactams by RCM and their evaluation against HIV protease |
Author: | Zaman, S. Campaner, P. Abell, A. |
Citation: | Bioorganic and Medicinal Chemistry, 2006; 14(24):8323-8331 |
Publisher: | Pergamon-Elsevier Science Ltd |
Issue Date: | 2006 |
ISSN: | 0968-0896 1464-3391 |
Statement of Responsibility: | Shazia Zaman, Pietro Campaner and Andrew D. Abell |
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. |
Keywords: | Ring-closing metathesis Lactams Diol HIV protease |
Description: | Copyright © 2006 Elsevier Ltd All rights reserved. |
DOI: | 10.1016/j.bmc.2006.09.009 |
Description (link): | http://www.elsevier.com/wps/find/journaldescription.cws_home/129/description#description |
Published version: | http://dx.doi.org/10.1016/j.bmc.2006.09.009 |
Appears in Collections: | Aurora harvest 6 Chemistry publications |
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