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Chemistry Education 2018 Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123 Page 40
August 27-28, 2018
Zurich, Switzerland
8th Edition of International Conference on
Chemistry Education
and Research
T here are four known subtypes of human adenosine receptors,
classified as A1, A2A, A2B and A3 adenosine receptors. They
regulate a large array of physiological and pathological functions
in the human body. Ligands targeting these adenosine receptor
subtypes have been reported to possess therapeutic potential
in various diseases. Of note, antagonists of the adenosine
receptor subtypes have been shown to be pharmacologically
beneficial inmodulating Alzheimer’s disease, Parkinson’s disease,
inflammatory disorders and cancer. Over the past decades,
medicinal chemists have strived to synthesize and characterize
new derivatives as human adenosine receptor antagonists with
biological activities of interest. In particular, our research group
has been working on the rational design, structural optimization
and characterization of new compounds acting as potent human
A3 and A2A adenosine receptor antagonists. These compounds
have displayed good binding affinities ranging from nanomolar
to low micromolar. In this paper, structural modification of new
derivatives based on tricyclic scaffold template, and subsequent
transition to the design of new compounds with bicyclic scaffold
will be discussed in details. In addition, molecular modeling
studies, such as molecular docking and quantitative structure-
activity relationship analysis performed in tandem to rationalize
the binding affinity profiles obtained from the pharmacological
studieswill alsobeelaborated. Inbrief, the integrationofmedicinal
chemistry, pharmacology and computational approaches
employed has led to the identification of potent and selective
human adenosine receptors antagonists.
Biography
Dr Cheong Siew Lee has obtained her degree in Pharmacy and PhD in Me-
dicinal Chemistry from the National University of Singapore, Singapore. She
has then undergone her postdoctoral training at the Institut für Pharmakolo-
gie, Universität Würzburg, Germany. Currently, she works as a lecturer at the
Department of Pharmaceutical Chemistry, International Medical University,
Malaysia. Her research interests revolve mainly around structural optimiza-
tion of new ligands targeting adenosine receptors and dopamine receptors
as well as application of computational approaches and pharmacological
characterization in the drug design and discovery. Her research work has
been published in various top international peer-reviewed journals and book
chapters.
Rational design of new ligands as human adenosine receptor
antagonists: Transition from tricyclic to bicyclic scaffold-
based derivatives
Cheong Siew Lee1, Pastorin Giorgiab 2, Spalluto Giampieroc3 and Klotz K-Nd 4
1International Medical University, Malaysia
2National University of Singapore, Singapore
3Università degli Studi di Trieste, Italy
4Universität Würzburg, Germany
Cheong Siew Lee et al., J Org Inorg Chem 2018, Volume 4
DOI: 10.21767/2472-1123-C5-014