| Title : Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors - Xing_2013_Eur.J.Med.Chem_63C_95 |
| Author(s) : Xing W , Fu Y , Shi Z , Lu D , Zhang H , Hu Y |
| Ref : Eur Journal of Medicinal Chemistry , 63C :95 , 2013 |
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Abstract :
2,6-Disubstituted pyridazinone 4 was identified by HTS as a novel acetylcholinesterase (AChE) inhibitor. Under SAR development, compound 17e stood out as displaying high AChE inhibitory activity and AChE/butyrylcholinesterase (BCHE) selectivity in vitro. Docking studies revealed that 17e might interact with the catalytic active site (CAS) and the peripheral anionic site (PAS) simultaneously. Based on this novel binding information, 6-ortho-tolylamino and N-ethyl-N-isopropylacetamide substituted piperidine were disclosed as new PAS and CAS binders. |
| PubMedSearch : Xing_2013_Eur.J.Med.Chem_63C_95 |
| PubMedID: 23466605 |
Xing W, Fu Y, Shi Z, Lu D, Zhang H, Hu Y (2013)
Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors
Eur Journal of Medicinal Chemistry
63C :95
Xing W, Fu Y, Shi Z, Lu D, Zhang H, Hu Y (2013)
Eur Journal of Medicinal Chemistry
63C :95