| dc.description.abstract | The nine new imidazole-hydrazone derivatives of Schiff base
were synthesized from the condensation reactions of 1-methyl1H-imidazole-2-carbaldehyde
with various substitutedhydrazide
derivatives. Structures of the final compounds (1a–
1i) were characterized by using
1
HNMR,
13
CNMR spectroscopic
techniques, elemental analysis, and crystal X-ray diffraction. The
in vitro carbonic anhydrase I and II potentials of these
synthesized were evaluated. The result suggests that compound
1a, a 4-methoxy substituted analog with an IC
of 0.949 μM,
was found to have the most potent hCA I inhibitory activity.
Compounds 1c, 1d, and 1h were the most potent compounds
50
on hCA II with IC
50
values of 3.330, 4.454, and 5.66 μM,
respectively. All compounds were examined for their cytotoxicity
towards human colorectal adenocarcinoma cell (HT29) and
rat glioma cell line (C6) compared to mouse fibroblast normal
cell line (L929) using the MTT assay method. The compounds
1a, 1d, and 1i exhibited significant antiproliferative activity
with less toxicity to a health cell line. Consequently, compound
1a could be the potential lead for emerging selective cytotoxic
compounds directing hCA I. Compound 1d could be the
potential lead for emerging selective cytotoxic compounds
directing hCA II. | tr |
