Abstract
6-Benzofuryl-, styryl, benzyl, and furfurylpurines as well as 6-[1(3H)-isobenzofuranylidenemethyl]purines have been synthesized and their activities against Mycobacterium tuberculosis (Mtb) determined. Several compounds displayed profound antimycobacterial activity in combination with low toxicity towards mammalian cells. NMR and X-ray crystallography were employed to determine the detailed structures and the results were supported by quantum chemical calculations.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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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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Cell Survival / drug effects
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Chlorocebus aethiops
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Crystallography, X-Ray
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Microbial Sensitivity Tests
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Models, Molecular
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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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Structure-Activity Relationship
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Tuberculosis / drug therapy*
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Vero Cells
Substances
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Antitubercular Agents
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Purines