Synthesis, characterization, antiamoebic activity and toxicity of novel bisdioxazole derivatives

European Journal of Medicinal Chemistry
2009.0

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 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.

Knowledge Graph

Similar Paper

Synthesis, characterization, antiamoebic activity and toxicity of novel bisdioxazole derivatives
European Journal of Medicinal Chemistry 2009.0
New derivatives of 3,5-substituted-1,4,2-dioxazoles: Synthesis and activity against Entamoeba histolytica
European Journal of Medicinal Chemistry 2009.0
Novel terpene based 1,4,2-dioxazoles: Synthesis, characterization, molecular properties and screening against Entamoeba histolytica
European Journal of Medicinal Chemistry 2011.0
New dioxazole derivatives: Synthesis and effects on the growth of Entamoeba histolytica and Giardia intestinalis
European Journal of Medicinal Chemistry 2010.0
Bis-pyrazolines: Synthesis, characterization and antiamoebic activity as inhibitors of growth of Entamoeba histolytica
European Journal of Medicinal Chemistry 2009.0
Synthesis of some 1,3,4-thiadiazole derivatives as inhibitors of Entamoeba histolytica
Medicinal Chemistry Research 2013.0
Synthesis, characterization, antiamoebic activity and cytotoxicity of novel 2-(quinolin-8-yloxy) acetohydrazones and their cyclized products (1,2,3-thiadiazole and 1,2,3-selenadiazole derivatives)
European Journal of Medicinal Chemistry 2010.0
Synthesis, characterization, antiamoebic activity and cytotoxicity of novel series of pyrazoline derivatives bearing quinoline tail
European Journal of Medicinal Chemistry 2010.0
Synthesis and in vitro evaluation of new ethyl and methyl quinoxaline-7-carboxylate 1,4-di-N-oxide against Entamoeba histolytica
Bioorganic & Medicinal Chemistry 2013.0
Synthesis, characterization and antiamoebic activity of some hydrazone and azole derivatives bearing pyridyl moiety as a promising heterocyclic scaffold
European Journal of Medicinal Chemistry 2012.0