Design, synthesis, molecular docking, and cholinesterase inhibitory potential of phthalimide-dithiocarbamate hybrids as new agents for treatment of Alzheimer's disease.

Design, synthesis, molecular docking, and cholinesterase inhibitory potential of phthalimide-dithiocarbamate hybrids as new agents for treatment of Alzheimer's disease.
Chem Biodivers. 2019 Sep 15;:
Authors: Mahdavi M, Asadi M, Ebrahimi M, Mohammadi-Khanaposhtani M, Azizian H, Sepehri S, Nadri H, Biglar M, Amanlou M, Larijani B, Mirzazadeh R, Edraki N
Abstract
A novel series of phthalimide-dithiocarbamate hybrids was synthesized and evaluated for 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. In silico docking study of the compounds 7g and 7h, respectively in the active site of AChE and BuChE revealed that these compounds bound to important residues. The compound 7g also showed remarkable neuroprotective activity comparable to the standard agent quercetin. Furthermore, compounds 7g and 7h possessed drug-like properties and were able to cross the BBB.
PMID: 31523926 [PubMed - as supplied by publisher]

Source: Chemistry and Biodiversity - September 14, 2019 Category: Biochemistry Authors: Mahdavi M, Asadi M, Ebrahimi M, Mohammadi-Khanaposhtani M, Azizian H, Sepehri S, Nadri H, Biglar M, Amanlou M, Larijani B, Mirzazadeh R, Edraki N Tags: Chem Biodivers Source Type: research