Synthesis, characterization, antiamoebic activity and toxicity of novel bisdioxazole derivatives.
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 microM), 4 (IC(50)=1.41 microM), 7 (IC(50)=1.05 microM) and 10 (IC(50)=1.01 microM) exhibited better antiamoebic activity than the standard drug metronidazole (IC(50)=1.80 microM). 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 microg/ml.
Iqbal
Prince Firdoos
PF
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Parveen
Humaira
H
Bhat
Abdul Roouf
AR
Hayat
Faisal
F
Azam
Amir
A
D000563:Amebicides / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001554:Benzene / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004748:Entamoeba histolytica / Q000187:drug effects*; D004749:Entamoebiasis / Q000188:drug therapy*; D020128:Inhibitory Concentration 50; D032386:Myoblasts, Cardiac / Q000166:cytology / Q000187:drug effects; D010080:Oxazoles / Q000737:chemistry* / Q000494:pharmacology*; D021261:Parasitic Sensitivity Tests; D051381:Rats; D013329:Structure-Activity Relationship
D000563:Amebicides; D010080:Oxazoles; D001554:Benzene