Abstract
In the present work, we synthesized a series of thiosemicarbazones derived from 1-indanones with good anti-Trypanosoma cruzi activity. Most of them displayed remarkable trypanosomicidal activity. All the compounds showed nonspecific cytotoxicity on human erythrocytes. The ability of the new compounds to inhibit cruzipain, the major cysteine protease of T. cruzi, was also explored. Thiosemicarbazones 12 and 24 inhibited this enzyme at the dose assayed. This interaction was also studied in terms of molecular docking.
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 Endopeptidases / metabolism
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Cysteine Proteinase Inhibitors / chemistry*
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Cysteine Proteinase Inhibitors / pharmacology
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Erythrocytes / drug effects
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Humans
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Indans / chemistry*
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Indans / pharmacology*
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Models, Molecular
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Molecular Conformation
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Protozoan Proteins
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Thiosemicarbazones / chemistry*
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Thiosemicarbazones / pharmacology*
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Trypanocidal Agents / chemistry*
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Trypanocidal Agents / pharmacology
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Trypanosoma cruzi / drug effects*
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Trypanosoma cruzi / enzymology
Substances
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Cysteine Proteinase Inhibitors
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Indans
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Protozoan Proteins
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Thiosemicarbazones
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Trypanocidal Agents
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Cysteine Endopeptidases
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cruzipain