131611-00-2Relevant academic research and scientific papers
Synthesis and anti-HIV-1 activity of N-hydroxy-N1-aminoguanidines
Doubell,Oliver
, p. 65 - 69 (2007/10/02)
The synthesis of 13 new Schiff bases of N-hydroxy-N1-aminoguanidines (1-13) starting from thiosemicarbazide are reported. These new derivatives were for the first time tested against infection by the Human Immunodeficiency Virus Type 1 (HIV-1) using the human T-lymphocyte cell line. Four N-hydroxy-N1-aminoguanidines (3, 4, 8 and 11) exhibited HIV-I inhibition in the micromolar range. The most active compound, [1-(1'-chloro-2'-hydroxy-3'-methoxybenzylidene)amino]-3-hydroxyguanidi ne(11) inhibited HIV-1 by 96% at 10 μg/ml concentration. All the derivatives exhibited substantial cytotoxicity at 320 μg/ml concentration. The results indicate that the activity against HIV-1 increases with increasing hydrophobicity and substituents with electron-donating properties.
