Design, synthesis, and biological evaluation of imidazo[1,2-a] pyridine derivatives as acetylcholinesterase inhibitors

Article · January 2010with9 Reads
Source: DOAJ

To explore novel and effective drugs for the treatment of Alzheimers disease(AD), a series of inhibitors of acetylcholineterase (AChE) were designed based on the Structure-based generation of a novel series of AchE inhibitors were carried out with crystal structure of acetylcholine esterase complexed with choline (PDB: 2HA3) obtained from protein data. Among synthesized inhibitor 7(a-e) exhibited good potency in enzyme inhibitory potency AChE: IC= 55 ± 0.53M, 73 ± 0.37M, and 51 ± 0.37M, 73 ± 0.40M, 48±0.75M, 7b and 7C also showed moderate to good activity in acetylcholinesterase assay in vitro using different sources of acetylcholinesterase studied (rat brain, human serum and electrical eel).