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Synthesis and Structure-Activity Relationship Study of Benzofuran-Based Chalconoids Bearing Benzylpyridinium Moiety As Potent Acetylcholinesterase Inhibitors Publisher Pubmed



Mostofi M1 ; Mohammadi Ziarani G1 ; Mahdavi M2 ; Moradi A3 ; Nadri H3 ; Emami S4 ; Alinezhad H5 ; Foroumadi A2 ; Shafiee A2
Authors
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Authors Affiliations
  1. 1. Department of Chemistry, Alzahra University, Vanak Square, Tehran, Iran
  2. 2. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medicinal Sciences, Tehran, Iran
  3. 3. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran
  4. 4. Department of Medicinal Chemistry, Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran
  5. 5. Faculty of Chemistry, University of Mazandaran, Babolsar, Iran

Source: European Journal of Medicinal Chemistry Published: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 μM was as potent as standard drug donepezil. © 2015 Elsevier Masson SAS. All rights reserved.