William N. Charman

TL;DR: The results were in contrast to the suggested hypothesis since the QT interval was reduced (and not increased) after halofantrine administration to hyperlipidaemic rabbits relative to fasted rabbits, suggesting it is unlikely that lipoprotein‐based uptake of hal ofantrine into the myocardium is a major contributor to the previously observed increase in QT prolongation after post‐prandial administration.

TL;DR: The alanine, glycine, leucine, lysine, and phenylalanine derivatives of dapsone all exhibited greater aqueous solubility, as their salts, than the parent compound.

TL;DR: New fluoroart Artemisinin derivatives containing polar or water-soluble functionalities at C-16 (11a-j, 12a-g) were synthesized using the key intermediate 16-bromo-10-trifluoromethyl anhydrodihydroartemisinin 10, and among them, amines 11a-c appeared to be highly in vivo efficient antimalarials on mice infected with Plasmodium berghei.

TL;DR: The present study describes the medicinal chemistry campaign that led to the development of the lead candidate, 3, highlighting the key structural features considered as critical for binding.