Abstract
Cyclization of benzene-1,4-dicarbaldehyde dioxime
1 with different aromatic aldehydes in inert atmosphere yielded the corresponding new bisdioxazoles
2–
11. The structure of
2–
11 was elucidated by spectral data.
In vitro antiamoebic activity was performed against HM1:IMSS strain of
Entamoeba histolytica. The results showed that the compounds
3 (IC
50
=
1.22
μM),
4 (IC
50
=
1.41
μM),
7 (IC
50
=
1.05
μM) and
10 (IC
50
=
1.01
μM) exhibited better antiamoebic activity than the standard drug metronidazole (IC
50
=
1.80
μM). The compounds
3,
4,
7 and
10 were tested for toxicity by MTT assay on H9c2 cardiac myoblasts and the results showed that the compounds
3,
4,
7 and
10 offered remarkable viability of 96.2%, 83.5%, 82% and 89%, respectively at a concentration of 12.5
μg/ml.
Novel bisdioxazoles
2–
11 were synthesized. Compounds
3,
4,
7 and
10 exhibited better antiamoebic activity and screened for toxicity.
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