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  • Exogenous micro-RNA and antagomir modulate osteogenic gene expression in tenocytes EXPERIMENTAL CELL RESEARCH Xiao, M., Iglinski-Benjamin, K. C., Sharpe, O., Robinson, W. H., Abrams, G. D. 2019; 378 (2): 119–23
  • Increased Prevalence of Concomitant Psychiatric Diagnoses Among Patients Undergoing Hip Arthroscopic Surgery ORTHOPAEDIC JOURNAL OF SPORTS MEDICINE Iglinski-Benjamin, K. C., Xiao, M., Safran, M. R., Abrams, G. D. 2019; 7 (1)
  • Design and synthesis of new piperidone grafted acetylcholinesterase inhibitors BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Basiri, A., Xiao, M., McCarthy, A., Dutta, D., Byrareddy, S. N., Conda-Sheridan, M. 2017; 27 (2): 228–31

    Abstract

    Alzheimer's disease (AD) is a neurodegenerative disorder affecting 35million people worldwide. A common strategy to improve the well-being of AD patients consists on the inhibition of acetylcholinesterase with the concomitant increase of the neurotransmitter acetylcholine at cholinergic synapses. Two series of unreported N-benzylpiperidines 5(a-h) and thiazolopyrimidines 9(a-q) molecules were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) inhibitory activities. Among the newly synthesized compounds, 5h, 9h, 9j, and 9p displayed higher AChE enzyme inhibitory activities than the standard drug, galantamine, with IC50 values of 0.83, 0.98, and 0.73μM, respectively. Cytotoxicity studies of 5h, 9h, 9j, 9n and 9p on human neuroblastoma cells SH-SY5Y, showed no toxicity up to 40μM concentration. Molecular docking simulations of the active compounds 5h and 9p disclosed the crucial role of π-π-stacking in their binding interaction to the active site AChE enzyme. The presented compounds have potential as AChE inhibitors and potential AD drugs.

    View details for DOI 10.1016/j.bmcl.2016.11.065

    View details for Web of Science ID 000392558500022

    View details for PubMedID 27914796

    View details for PubMedCentralID PMC5518470