SYNTHESIS AND ACETYLCHOLINESTERASE/BUTYRYLCHOLINESTERASE INHIBITION ACTIVITY OF ARECOLINE-, 4-THIAZOLIDINONE- AND PIPERIDINE- BASED CONJUGATES

Authors

  • Kothanahally Shivaramu Sharath Kumar Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore-570006
  • Chakrabhavi Dhananjaya Mohan Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore-570006
  • Swamy Jagadish Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore-570006
  • KODAGAHALLI SATHYA Rakesh Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore-570006
  • Ananda Hanumappa Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysore-570006
  • Basappa Department of chemistry, Bangalore University, Bangalore
  • KANCHUGARAKOPPAL SUBBEGOWDA Rangappa Department of Studies in Chemistry, University of Mysore, Mysore

Abstract

Objective: The aim of the study is to design, synthesize and identification of novel acetylcholinesterase/butyrylcholinesterase (AChE/BuChE)
inhibitors.
Methods: The AChE and BuChE inhibition activity of a library of piperidine and 4-thiazolidinone substituted arecoline derivatives are described. The
chemical structures of newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectral analysis.
Results: The cholinesterase inhibition assays indicated that few of the synthesized compounds exhibited considerable activity at micromolar range
for AChE over BuChE. Compound 7c exhibited the most potent AChE inhibitory activity with an IC50 value of 6.62 μM for AChE and 13.78 μM for BuChE,
which is comparable to the standard Neostigmine with an IC50 2.05 μM for AChE and 3.64 μM for BuChE respectively.
Conclusion: Our results clearly demonstrate that arecoline-4-thiazolidinone derivatives open up a new avenue in the field of Alzheimer's disease.

Keywords: Arecoline analogs, Propylphosphonic anhydride (T3P®), Acetylcholinesterase/butyrylcholinesterase inhibitor, 4-thiazolidinones.

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Published

01-01-2015

How to Cite

Sharath Kumar, K. S., C. D. Mohan, S. Jagadish, K. S. Rakesh, A. Hanumappa, Basappa, and K. S. . Rangappa. “SYNTHESIS AND ACETYLCHOLINESTERASE/BUTYRYLCHOLINESTERASE INHIBITION ACTIVITY OF ARECOLINE-, 4-THIAZOLIDINONE- AND PIPERIDINE- BASED CONJUGATES”. Asian Journal of Pharmaceutical and Clinical Research, vol. 8, no. 1, Jan. 2015, pp. 142-8, https://journals.innovareacademics.in/index.php/ajpcr/article/view/2619.

Issue

Vol 8 Issue 1 (January-February) 2015

Section

Original Article(s)

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