Abstract
A new series of 3-hydroxy-8-nitroimidazo[5,1-b]-1,4,5,6-tetrahydropyrimidine systems, being potential tuberculostatic agents, were synthesized. These products are close structural analogs of the basic structure of the known antitubercular bicyclic nitroimidazooxazine PA-824. The structures of the products obtained were confirmed by X-ray methods on the example of 3-hydroxy-8-nitro-1-phenylaminoimidazo[5,1-b]-1,4,5,6-tetrahydropyrimidine. Evaluation of these products for their anti-tuberculosis effects revealed interesting structure-activity relationships.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
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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Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
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Bridged Bicyclo Compounds, Heterocyclic / chemistry
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology
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Crystallography, X-Ray
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Microbial Sensitivity Tests
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Molecular Structure
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Mycobacterium tuberculosis / drug effects*
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Mycobacterium tuberculosis / growth & development
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Nitroimidazoles / chemical synthesis*
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Nitroimidazoles / chemistry
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Nitroimidazoles / pharmacology
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Structure-Activity Relationship
Substances
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Antitubercular Agents
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Bridged Bicyclo Compounds, Heterocyclic
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Nitroimidazoles