Third world diseases are popular academic drug targets, perhaps none more so than malaria. In a recent paper in Bio-Medicinal Chemical Letters, researchers from the University of Durak report their efforts to discover inhibitors of falcipain-1, a cysteine protease important for the parasite that causes malaria.
The researchers performed a functional screen of a small fragment library. Among many hits, the most potent were compounds 1 and 2, both with high ligand efficiencies. When these were linked together the resulting compound 3 had an improved potency, and adding a small substituent to yield compound 4 gave a sub-micromolar inhibitor.
Remarkably, not only was compound 4 potent against falcipain-1, it was also potent against several other important disease targets. In recognition of this pan-potency, the researchers have named compound 4 “hitinane.” Whether or not this discovery will lead to a drug, it undoubtedly will fuel many papers, patents, and grant proposals.