Abstract
A series of new arylamino quinoline derivatives was designed based on the quinine and mefloquine scaffolds and evaluated in vitro for antiplasmodial and antimycobacterial activities. A number of these compounds exhibited significant activity against the drug-sensitive 3D7 and drug-resistant K1 strains of Plasmodium falciparum. Furthermore, two compounds, 4.12b and 4.12d, also showed 94 and 98% growth inhibitory activity against non-replicating and replicating Mycobacterium tuberculosis strains, respectively.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aminoquinolines / chemical synthesis*
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Aminoquinolines / pharmacology
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Antiprotozoal Agents / chemical synthesis*
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Antiprotozoal Agents / pharmacology
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Antitubercular Agents / chemical synthesis*
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Antitubercular Agents / pharmacology
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Biological Assay
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Blood-Brain Barrier / metabolism
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Computer Simulation
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Drug Design
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Erythrocytes / drug effects
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Erythrocytes / parasitology
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Humans
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Inhibitory Concentration 50
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Mefloquine / chemistry
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Mefloquine / pharmacology
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Microbial Sensitivity Tests
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Models, Biological
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Mycobacterium tuberculosis / drug effects*
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Mycobacterium tuberculosis / growth & development
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Plasmodium falciparum / drug effects*
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Plasmodium falciparum / growth & development
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Quinine / chemistry
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Quinine / pharmacology
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Structure-Activity Relationship
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Tetrazoles / chemical synthesis*
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Tetrazoles / pharmacology
Substances
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Aminoquinolines
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Antiprotozoal Agents
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Antitubercular Agents
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Tetrazoles
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Quinine
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Mefloquine