<abstract xmlns="http://www.w3.org/1999/xhtml"><p>Synthesis and biological evaluation of a series (N = 16) of cyclic and acyclic hydroxyurea derivatives, including benzotriazole-, isocyanuric acid- and biuret-containing compounds, are disclosed. 1-N-(benzyloxycarbamoyl)benzotriazole was used as a benzyloxyisocyanate donor, a useful intermediate in the preparation of substituted hydroxyurea. Antibacterial activities of synthesized hydroxyurea derivatives were tested on three E. coli strains, i.e., a strain susceptible to antibiotics, a strain resistant to macrolide antibiotics and a strain resistant to aminoglycoside antibiotics. Six compounds (three acyclic and three cyclic hydroxyureas) showed growth inhibition of the tested E. coli strains, with different specificity toward each strain. Results of the cytotoxic activity evaluation revealed that twelve out of sixteen test compounds were cytotoxic to human acute monocytic leukemia THP-1 and/or human acute T cell leukemia Jurkat cell line. 1-(N-hydroxycarbamoyl) benzotriazole () increased the metabolic activity of both cell lines. Two compounds, 1-(N-hydroxycarbamoyl) benzotriazole (<bold>5</bold>) and N,N’,N’’-trihydroxybiuret (<bold>15</bold>), were identified as potential NO donors.</p></abstract>

Synthesis and biological evaluation of a series (N = 16) of cyclic and acyclic hydroxyurea derivatives, including benzotriazole-, isocyanuric acid- and biuret-containing compounds, are disclosed. 1-N-(benzyloxycarbamoyl)benzotriazole was used as a benzyloxyisocyanate donor, a useful intermediate in the preparation of substituted hydroxyurea. Antibacterial activities of synthesized hydroxyurea derivatives were tested on three E. coli strains, i.e., a strain susceptible to antibiotics, a strain resistant to macrolide antibiotics and a strain resistant to aminoglycoside antibiotics. Six compounds (three acyclic and three cyclic hydroxyureas) showed growth inhibition of the tested E. coli strains, with different specificity toward each strain. Results of the cytotoxic activity evaluation revealed that twelve out of sixteen test compounds were cytotoxic to human acute monocytic leukemia THP-1 and/or human acute T cell leukemia Jurkat cell line. 1-(N-hydroxycarbamoyl) benzotriazole () increased the metabolic activity of both cell lines. Two compounds, 1-(N-hydroxycarbamoyl) benzotriazole (5) and N,N’,N’’-trihydroxybiuret (15), were identified as potential NO donors.

Synthesis, antibacterial and cytotoxic activity evaluation of hydroxyurea derivatives

University of Zagreb Faculty of Pharmacy and Biochemistry Zagreb, Croatia

Acta Pharmaceutica

Synthesis and biological evaluation of a series (N = 16) of cyclic and acyclic hydroxyurea derivatives, including benzotriazole-, isocyanuric acid- and...

Synthesis, antibacterial and cytotoxic activity evaluation of hydroxyurea derivatives

Publié en ligne: 10 juil. 2013

Pages: 175 - 191

DOI: https://doi.org/10.2478/acph-2013-0014

Mots clés
hydroxyurea derivatives, synthesis, antibacterial activity, cytotoxicity

This content is open access.

Synthesis, antibacterial and cytotoxic activity evaluation of hydroxyurea derivatives

Publié en ligne: 10 juil. 2013

Pages: 175 - 191

DOI: https://doi.org/10.2478/acph-2013-0014

Mots cléshydroxyurea derivatives, synthesis, antibacterial activity, cytotoxicity

This content is open access.

Mots clés
hydroxyurea derivatives, synthesis, antibacterial activity, cytotoxicity