Novel terpene based 1,4,2-dioxazoles: Synthesis, characterization, molecular properties and screening against Entamoeba histolytica

Title
Novel terpene based 1,4,2-dioxazoles: Synthesis, characterization, molecular properties and screening against Entamoeba histolytica
Author(s)
최인호압둘루프바트Mohmmad Younus Wani[Mohmmad Younus Wani]Fareeda Athar[Fareeda Athar]Attar Salauddin[Attar Salauddin]Subhash Mohan Agarwa[Subhash Mohan Agarwa]Amir Azam[Amir Azam]
Keywords
ISOPRENOIDS PERILLYL ALCOHOL; DRUG DISCOVERY; ORAL BIOAVAILABILITY; ESSENTIAL OILS; DERIVATIVES; PREDICTION; PLANT; ELECTROPHORESIS; PERMEABILITY; CONSTITUENTS
Issue Date
201109
Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Citation
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.9, pp.4742 - 4752
Abstract
In present investigation a series of 20 dioxazole analogues (1-20) were synthesized, characterized and subjected to molecular properties prediction, anti-amoebic screening and cytotoxicity evaluation. Out of the twenty compounds viz. 3,5-substituted-1,4,2-dioxazoles, six compounds have shown IC50 values in the range (1.00-1.10 mu M) lower than the standard drug metronidazole (IC50 = 1.45 mu M). The toxicological studies of the active compounds on H9c2 rat cardiac myoblasts showed that all compounds were nontoxic. The pKa, and log P values have also been predicted. Compound 8 showed the most promising results based on anti-amoebic evaluation, cytotoxicity studies and physico-chemical properties prediction. (C) 2011 Elsevier Masson SAS. All rights reserved.
URI
http://hdl.handle.net/YU.REPOSITORY/24595http://dx.doi.org/10.1016/j.ejmech.2011.06.005
ISSN
0223-5234
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생명공학부 > 생명공학부 > Articles
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