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Wiley-VCH Verlag, ChemInform, 41(43), p. no-no, 2012

DOI: 10.1002/chin.201241175

Wiley, Archiv der Pharmazie, 6(345), p. 463-467, 2012

DOI: 10.1002/ardp.201100379

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ChemInform Abstract: Synthesis, Structure and Biological Evaluation of Novel Bicyclic Nitroimidazole Derivatives (III).

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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.