Abstract
6-Aryl- and 6-heteroaryl-9-benzylpurines have been synthesized employing palladium-catalyzed coupling reactions in the step forming the C-C or C-N bond between the aryl- or heteroaryl and the purine. The compounds were screened for activity against Mycobacterium tuberculosis as well as representative Gram+ and Gram- bacteria, and for cytotoxic effects on mammalian cells. Several potent antimycobacterials were identified. These compounds probably act by a novel and selective mechanism; they exhibit low toxicity toward other bacteria as well as mammalian cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / toxicity
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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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Antitubercular Agents / toxicity
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Cell Line
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Cell Proliferation / drug effects
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Chlorocebus aethiops
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Escherichia coli / drug effects
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Inhibitory Concentration 50
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Molecular Structure
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Mycobacterium tuberculosis / drug effects
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Purines / chemical synthesis
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Purines / chemistry*
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Purines / pharmacology*
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Staphylococcus aureus / drug effects
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Structure-Activity Relationship
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Vero Cells
Substances
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Antineoplastic Agents
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Antitubercular Agents
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Purines
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purine