Abstract
In the present paper, we report the synthesis via catalytic Michael reaction and biological results of a series of 3-heteryl substituted pyrrolidine-2,5-dione derivatives as moderate inhibitors against Mycobacterium tuberculosis H37Rv growth. Some of them present also inhibition activities against InhA.
Keywords:
InhA; Michael addition; Succinimide; Tuberculosis.
Copyright © 2013 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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Antitubercular Agents / chemical synthesis
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Antitubercular Agents / chemistry*
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Antitubercular Agents / pharmacology*
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Bacterial Proteins / antagonists & inhibitors*
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Bacterial Proteins / metabolism
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Humans
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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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Mycobacterium tuberculosis / growth & development
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Oxidoreductases / antagonists & inhibitors*
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Oxidoreductases / metabolism
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Pyrrolidines / chemical synthesis
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Pyrrolidines / chemistry*
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Pyrrolidines / pharmacology*
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Structure-Activity Relationship
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Tuberculosis / drug therapy
Substances
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Antitubercular Agents
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Bacterial Proteins
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Pyrrolidines
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Oxidoreductases
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InhA protein, Mycobacterium
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pyrrolidine