Title : Synthesis and structure-activity relationship study of benzofuran-based chalconoids bearing benzylpyridinium moiety as potent acetylcholinesterase inhibitors - Mostofi_2015_Eur.J.Med.Chem_103_361 |
Author(s) : Mostofi M , Mohammadi Ziarani G , Mahdavi M , Moradi A , Nadri H , Emami S , Alinezhad H , Foroumadi A , Shafiee A |
Ref : Eur Journal of Medicinal Chemistry , 103 :361 , 2015 |
Abstract :
A series of benzofuran-based chalconoids 6a-v were designed and synthesized as new potential AChE inhibitors. The in vitro assay of synthesized compounds 6a-v showed that most compounds had significant anti-AChE activity at micromolar or sub-micromolar levels. Among the tested compounds, 3-pyridinium derivative 6m bearing N-(2-bromobenzyl) moiety and 7-methoxy substituent on the benzofuran ring exhibited superior activity. This compound with IC50 value of 0.027 muM was as potent as standard drug donepezil. |
PubMedSearch : Mostofi_2015_Eur.J.Med.Chem_103_361 |
PubMedID: 26363872 |
Mostofi M, Mohammadi Ziarani G, Mahdavi M, Moradi A, Nadri H, Emami S, Alinezhad H, Foroumadi A, Shafiee A (2015)
Synthesis and structure-activity relationship study of benzofuran-based chalconoids bearing benzylpyridinium moiety as potent acetylcholinesterase inhibitors
Eur Journal of Medicinal Chemistry
103 :361
Mostofi M, Mohammadi Ziarani G, Mahdavi M, Moradi A, Nadri H, Emami S, Alinezhad H, Foroumadi A, Shafiee A (2015)
Eur Journal of Medicinal Chemistry
103 :361