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Updated: May 25, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, structure and biological evaluation of novel bicyclic nitroimidazole derivatives
Lucjusz Zaprutko1, Justyna Zwawiak, Ewa Augustynowicz-Kopeć
1Pharmaceutical Faculty, Chair and Department of Organic Chemistry, Poznan University of Medical Sciences, Poznań, Poland. zaprutko@ump.edu.pl
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.
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