Acta Pharmaceutica, Vol. 63 No. 2, 2013.
Izvorni znanstveni članak
https://doi.org/10.2478/acph-2013-0014
Synthesis, antibacterial and cytotoxic activity evaluation of hydroxyurea derivatives
IVAN KOS
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
MILENA JADRIJEVIĆ-MLADAR TAKAČ
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
IVAN BUTULA
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
MLADEN BIRUŠ
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
GORDANA MARAVIĆ-VLAHOVIČEK
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
SANJA DABELIĆ
; University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia
Sažetak
Synthesis and biological evaluation for a series (N = 16) of cyclic and acyclic hydroxyurea derivatives including benzotriazole-, isocyanuirc acid- and biuret-containing compounds, are disclosed. 1-N-(benzyloxycarbamoyl)benzotriazole was used as 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., strain susceptible to antibiotics, strain resistant to macrolide antibiotics and strain resistant to aminoglycoside antibiotics. Six compounds (three acyclic and three cyclic hydroxyureas) showed the growth inhibition of 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 on human acute T cell leukemia Jurkat cell line. 1-(N-hydroxycarbamoyl)benzotriazole (5) increased 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.
Ključne riječi
hydroxyurea derivatives; synthesis; antibacterial activity; cytotoxicity
Hrčak ID:
97696
URI
Datum izdavanja:
30.6.2013.
Posjeta: 1.764 *