Peter Mubanga Cheuka

TL;DR: This review highlights the potential that remains untapped in natural products as drug leads for NTDs, and covers natural products from plant, marine, and microbial sources including natural-product-inspired semi-synthetic derivatives which have been evaluated against the various causative agents of N TDs.

TL;DR: Future antimalarial drug discovery efforts seeking to identify plasmepin inhibitors should focus on incorporating non-haemoglobinase plasmepsins such as V, IX and X in their screening in order to maximise chances of success.

TL;DR: Cocrystallization and salt formation were used to produce new multicomponent forms of a novel antimalarial imidazopyridazine drug lead that displayed improved physicochemical properties that showed an improvement in the maximum concentrations attained by the drug lead and the rate at which it dissolved.

TL;DR: The synthesis and antiplasmodium evaluation of a new series of amidated analogues are reported and it is demonstrated that these compounds potently inhibit Plas modium phosphatidylinositol-4-kinase (PI4K) type IIIβ while moderately inhibiting cyclic guanidine monophosphate (cGMP)-dependent protein kinase (PKG) activity in vitro.

TL;DR: The synthesis and structure-activity relationship studies of new imidazopyridazines aimed at improving aqueous solubility and countering hERG inhibition while maintaining antiplasmodial potency are reported.