Abstract
Twenty-three naphthoimidazoles and six naphthoxazoles were synthesised and evaluated against susceptible and rifampicin- and isoniazid-resistant strains of Mycobacterium tuberculosis. Among all the compounds evaluated, fourteen presented MIC values in the range of 0.78 to 6.25 μg/mL against susceptible and resistant strains of M. tuberculosis. Five structures were solved by X-ray crystallographic analysis. These substances are promising antimycobacterial prototypes.
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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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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Azoles / chemical synthesis
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Azoles / chemistry
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Azoles / pharmacology*
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Cell Proliferation / drug effects
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Humans
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Imidazoles / chemical synthesis
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Leukocytes, Mononuclear / cytology
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Leukocytes, Mononuclear / drug effects
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Microbial Sensitivity Tests
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Models, Molecular
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Molecular Structure
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Mycobacterium tuberculosis / drug effects*
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Naphthoquinones / chemical synthesis
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Naphthoquinones / chemistry
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Naphthoquinones / pharmacology*
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Oxazoles / chemical synthesis
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Oxazoles / chemistry
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Oxazoles / pharmacology*
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Structure-Activity Relationship
Substances
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Antitubercular Agents
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Azoles
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Imidazoles
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Naphthoquinones
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Oxazoles