Research Area (Doctoral):
Alzheimer’s disease is the leading cause of dementia with an estimated cost to the economy of $259 billion in the USA in 2017 alone. The disease is multifaceted and a clear molecular genesis or cause of the disease has to date not been unambiguously proven. To date several hypotheses to target drug development have been proposed including the cholinergic, amyloid-beta, tau, calcium channel and inflammation hypotheses. Divan’s research focuses on the development of novel duel-inhibitors targeting the inhibition of acetyl choline clearance and aggregation of amyloid-beta through the inhibition of the catalytic triad and peripheral anionic site of acetyl cholinesterase. Research highlights include the development of structural analogues of the cholinesterase inhibitor Donepezil displaying nano-molar activity against acetylcholinesterase with no cytotoxicity against neuroblastoma cell lines and the development of methodologies for the synthesis of tri- and tetracyclic scaffolds for the use as duel-target inhibitors.
Dr Darren Riley, Dr Jenny-Lee Panayides and Prof. Vanessa Steenkamp
1. Targeting Alzheimer’s disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil.
D.G. van Greunen, W. Cordier, M. Nell, C. van der Westhuyzen, V. Steenkamp, J. Panayides, D.L. Riley. European Journal of Medicinal Chemistry 2017, 127, 671-690.
2015 – Neurosciences Day 2015 (University of Pretoria) “Investigations of previously unexplored chemical space surrounding the cholinesterase inhibitor Donepezil”
2015 – SWAAK conference (Bloemfontein) “Ondersoek na voorheen onderkende chemise ruimte rondom die asetielcholieneseterase inhibeerder Donepezil”
2016 – Neurosciences Day 2016 (University of Pretoria) “Targeting Alzheimer’s disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil”
2016 – Frank Warren (Rhodes University) “Utilization of Flow Chemistry for the Synthesis of the Cholinesterase Inhibitor Donepezil”
2016 – Frank Warren (Rhodes University) “Targeting Alzheimer’s Disease By Investigating Previously Unexplored Chemical Space Surrounding The Cholinesterase Inhibitor Donepezil” Poster Prize
2017 – Young Chemists Symposium (Tshwane University of Technology) “Functionalization of Previously Unexplored Chemical Space Surrounding The Cholinesterase Inhibitor Donepezil For Treatment of Alzheimer’s Disease” 1st Prize Presentation