Abstract
A series of 4-amino-7-chloroquinoline derivatives were synthesized by the reaction of 4,7-dichloro-quinoline with the corresponding diamine and then with propargyl bromide. In addition, platinum(II) complexes were obtained by reacting some of the organic derivatives with K(2)PtCl(4). Several of the synthesized compounds displayed antituberculosis activities. Compound 3 was 47.5 times more active than amphotericin B against Leishmania chagasi (IC(50)=0.04 μg/mL). Compounds 5, 6, 7, 9, 10, 11 and 13 presented promising results against Mycobacterium tuberculosis, with MIC values ranging from 12.5 to 15.6 μg/mL, comparable to the "first and second line" drugs used to treat tuberculosis.
Copyright © 2011 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 / chemistry
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Aminoquinolines / pharmacology*
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Amphotericin B / pharmacology
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Antitubercular Agents / chemical synthesis*
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Antitubercular Agents / chemistry
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Antitubercular Agents / pharmacology
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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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Diamines / chemistry
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Leishmania / drug effects*
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Microbial Sensitivity Tests / methods
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Mycobacterium tuberculosis / drug effects
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Pargyline / analogs & derivatives
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Pargyline / chemistry
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Platinum / chemistry*
Substances
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Aminoquinolines
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Antitubercular Agents
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Coordination Complexes
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Diamines
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Platinum
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Amphotericin B
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Pargyline
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propargyl bromide
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4-aminoquinoline