Abstract
Picking a fight with parasites! Trypanothione reductase (TR) is a validated drug target for the development of antileishmanial agents. A group of structurally diverse gold-containing compounds was evaluated in vitro for TR inhibition. A number of compounds exhibited potent activity and deserve further pharmacological evaluation.
Keywords:
Leishmania; antiprotozoal agents; gold; inhibitors; trypanothione reductase.
Copyright © 2013 WILEY‐VCH Verlag GmbH & Co. KGaA, Weinheim.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antiprotozoal Agents / chemical synthesis
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Antiprotozoal Agents / chemistry*
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Antiprotozoal Agents / pharmacology
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Catalytic Domain
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Coordination Complexes / chemical synthesis
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Coordination Complexes / chemistry*
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Coordination Complexes / pharmacology
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Crystallography, X-Ray
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology
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Gold / chemistry*
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Kinetics
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Leishmania / drug effects
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Leishmania / enzymology
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Molecular Docking Simulation
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NADH, NADPH Oxidoreductases / antagonists & inhibitors*
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NADH, NADPH Oxidoreductases / metabolism
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Protein Binding
Substances
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Antiprotozoal Agents
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Coordination Complexes
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Enzyme Inhibitors
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Gold
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NADH, NADPH Oxidoreductases
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trypanothione reductase