Crystal Growth, Single Crystal Structure, and Biological Activity of Thiazolo-Pyridine Dicarboxylic Acid Derivatives

摘要

Four novel TPDCA derivatives were prepared via a supersaturation method combining TPDCA with water, N -methyl-2-pyrrolidone (NMP), Na(PO_(2)H_(2)), and ammonia solution: 2(C_(9)H_(7)NO_(5)S)H_(2)O (1 ), (C_(9)H_(7)NO_(5)S)C_(5)H_(9)NO (2 ), (C_(9)H_(7)NO_(5)S)Na(PO_(2)H_(2)) (3 ), and (C_(9)H_(5)NO_(5)S)(NH_(4))_(2)(H_(2)O) (4 ). Their crystal structures were determined by single-crystal X-ray diffraction. Compounds (1 ) and (2 ) crystallize in the monoclinic space groups P 2_(1) and P 2_(1)/c , respectively, whereas compounds (3 ) and (4 ) crystallize in the triclinic space group P 1?. Weak and moderate hydrogen bonds were detected in the four compounds. In the biological tests, (1 ) and (3 ) exhibited significant antibacterial activity against Escherichia coli and Staphylococcus aureus ; in addition, (1 ) was cytotoxic against leukemia HL-60 cells with the IC_(50) value of 158.5 ± 12.5 μM.