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We have synthesized benzo[ d ]oxazole derivatives ( 1–21 ) through a multistep reaction. Alteration in the structure of derivatives was brought in the last step  via  using various substituted aromatic aldehydes. In search of an anti-Alzheimer agent, all derivatives were evaluated against acetylcholinesterase and butyrylcholinesterase enzyme under positive control of standard drug donepezil (IC 50  = 0.016 ± 0.12 and 4.5 ± 0.11 µM) respectively. In case of acetylcholinesterase enzyme inhibition, derivatives  8 ,  9  and  18  (IC 50  = 0.50 ± 0.01, 0.90 ± 0.05 and 0.3 ± 0.05 µM) showed very promising inhibitory potentials. While in case of butyrylcholinesterase enzyme inhibition, most of the derivatives like  6, 8, 9, 13, 15, 18  and  19  (IC 50  = 2.70 ± 0.10, 2.60 ± 0.10, 2.20 ± 0.10, 4.25 ± 0.10, 3.30 ± 0.10, 0.96 ± 0.05 and 3.20 ± 0.10 µM) displayed better inhibitory potential than donepezil. Moreover, derivative  18  is the most potent one among the series in both inhibitions. The binding interaction of derivatives with the active gorge of the enzyme was confirmed  via  a docking study. Furthermore, the binding interaction between derivatives and the active site of enzymes was correlated through the SAR study. Structures of all derivatives were confirmed through spectroscopic techniques such as  1 H-NMR,  13 C-NMR and HREI-MS, respectively. Communicated by Ramaswamy H. Sarma

Synthesis, in vitro biological screening and docking study of benzo[ d ]oxazole bis Schiff base derivatives as a potent anti-Alzheimer agent