Abstract
We report herein, design and synthesis of vinylaminophosphonates, a novel class of compounds as possible cysteine protease inhibitors. The synthesis of vinylaminophosphonates has been accomplished employing Tsuji-Trost reaction as a key step. The synthesized compounds were assayed against papain, a model cysteine protease and some of our synthesized compounds showed IC(50) values in the range of 30-54 μM thereby suggesting that these chemical entities thus could constitute an interesting template for the design of potential novel protease inhibitors.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cysteine Proteinase Inhibitors / chemical synthesis
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Cysteine Proteinase Inhibitors / chemistry*
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Cysteine Proteinase Inhibitors / pharmacology
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Humans
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Models, Molecular
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Molecular Structure
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Organophosphonates / chemical synthesis
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Organophosphonates / chemistry*
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Organophosphonates / pharmacology*
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Peptides / chemical synthesis
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Peptides / chemistry*
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Peptides / pharmacology*
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Spectroscopy, Fourier Transform Infrared
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Structure-Activity Relationship
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Vinyl Compounds / chemical synthesis
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Vinyl Compounds / chemistry
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Vinyl Compounds / pharmacology
Substances
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Cysteine Proteinase Inhibitors
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Organophosphonates
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Peptides
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Vinyl Compounds