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Synthesis and anticholinesterase activity of new substituted benzo[ d ]oxazole‐based derivatives
Author(s) -
Pouramiri Behjat,
Moghimi Setareh,
Mahdavi Mohammad,
Nadri Hamid,
Moradi Alireza,
TavakolinejadKermani Esmat,
Firoozpour Loghman,
Asadipour Ali,
Foroumadi Alireza
Publication year - 2017
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12902
Subject(s) - butyrylcholinesterase , oxazole , acetylcholinesterase , chemistry , aché , stereochemistry , docking (animal) , ic50 , in vitro , cholinesterase , enzyme , combinatorial chemistry , biochemistry , pharmacology , biology , medicine , nursing
A series of novel benzo[ d ]oxazole derivatives ( 6a–n ) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases ( AC hE) and butyrylcholinesterase ( BC hE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinesterase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AC hE and BC hE activities with IC 50 values of 1.03–1.35 and 6.6–8.1 μ m , respectively. Docking studies also provided the binding modes of action and identified hydrophobic pi forces as the main interaction.