Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking

Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series o...

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Detalles Bibliográficos
Autores principales: Yar, Muhammad, Bajda, Marek, Mehmood, Rana Atif, Sidra, Lala Rukh, Ullah, Nisar, Shahzadi, Lubna, Ashraf, Muhammad, Ismail, Tayaba, Shahzad, Sohail Anjum, Khan, Zulfiqar Ali, Naqvi, Syed Ali Raza, Mahmood, Nasir
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers Ltd 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3977535/
https://www.ncbi.nlm.nih.gov/pubmed/24719609
http://dx.doi.org/10.2174/15701808113106660078
Descripción
Sumario:Cholinesterases (ChEs) play a vital role in the regulation of cholinergic transmission. The inhibition of ChEs is considered to be involved in increasing acetylcholine level in the brain and thus has been implicated in the treatment of Alzheimer’s disease. We have designed and synthesized a series of novel indole derivatives and screened them for inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of the tested compounds exhibited inhibitory activity against AChE and BChE. Among them 4f and 6e showed the highest AChE inhibitory activity with IC(50) 91.21±0.06 and 68.52±0.04 μM, respectively. However compound 5a exhibited the highest inhibitory activity against BChE (IC(50) 55.21±0.12 μM).

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