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Design, Synthesis, Molecular Docking, and Cholinesterase Inhibitory Potential of Phthalimide-Dithiocarbamate Hybrids As New Agents for Treatment of Alzheimer's Disease Publisher Pubmed



Asadi M1 ; Ebrahimi M1 ; Mohammadikhanaposhtani M2 ; Azizian H3 ; Sepehri S4 ; Nadri H5 ; Biglar M6 ; Amanlou M1 ; Larijani B6 ; Mirzazadeh R7 ; Edraki N8 ; Mahdavi M6
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 1417653761, Iran
  2. 2. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, 4717647745, Iran
  3. 3. Department of Medicinal Chemistry, School of Pharmacy-International Campus, Iran University of Medical Sciences, Tehran, 14665354, Iran
  4. 4. Department of Medicinal Chemistry, School of Pharmacy, Ardabil University of Medical Sciences, Ardabil, 5618953141, Iran
  5. 5. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Shahid Sadoughi University of Medical Sciences, Yazd, 8915173160, Iran
  6. 6. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, 1417653761, Iran
  7. 7. Department of Biochemistry, Pasteur Institute of Iran, Tehran, 1316943551, Iran
  8. 8. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, 7134853734, Iran

Source: Chemistry and Biodiversity Published:2019


Abstract

A novel series of phthalimide-dithiocarbamate hybrids was synthesized and evaluated for in vitro inhibitory potentials against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The anti-cholinesterase results indicated that among the synthesized compounds, the compounds 7g and 7h showed the most potent anti-AChE and anti-BuChE activities, respectively. Molecular docking and dynamic studies of the compounds 7g and 7h, respectively, in the active site of AChE and BuChE revealed that these compounds as well interacted with studied cholinesterases. These compounds also possessed drug-like properties and were able to cross the BBB. © 2019 Wiley-VHCA AG, Zurich, Switzerland
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