Biological Evaluation of Halogenated Thioureas as Cholinesterases Inhibitors Against Alzheimer’s Disease & Molecular Modeling Studies

Author(s): Jamshed Iqbal, Sumera Zaib, Aamer Saeed, Muhammad Muddassar.

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 6 , 2015

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Abstract:

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition is thought to be an encouraging approach towards the therapy of Alzheimer’s disease (AD). The current paper targets to give a concise information of mono and dihalo- substituted thioureas similarity with anti-AD potential. The present results represent evaluation of cholinesterase inhibitory potential for halogenated thioureas derivatives. Compound 1t was constituted to be highly potent inhibitor with Ki value 0.12 ± 0.05 µM against AChE, while 1b was most the active inhibitor for BChE with Ki value of 0.03 ± 0.001 µM. Molecular docking simulations were performed using the homology models of both cholinesterases in order to explore the plausible binding modes of synthesized compounds.

Keywords: Acetylcholinesterase, alzheimer’s disease, butyrylcholinesterase, docking simulations, halogenated thioureas, homology models.

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Article Details

VOLUME: 12
ISSUE: 6
Year: 2015
Page: [488 - 494]
Pages: 7
DOI: 10.2174/1570180812666141201222247
Price: $65

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