Addressing the most neglected diseases through an open research model: the discovery of fenarimols as novel drug candidates for eumycetoma

by Lim W, Melse Y, Konings M, Phat Duong H, Eadie K, Laleu B, Perry B, Todd M, Ioset J-R, and van de Sande W. PLOS Neglected Tropical Diseases 2018, 12(4): e0006437, doi: 10.1371/journal.pntd.0006437ER.

Summary: The authors describe a study in which 800 diverse drug-like molecules were screened for activity against eumycetoma, 215 of which were active in vitro. One of the most potent compounds, a fenarimol analogue for which a large analogue library is available, led to the screening of an additional 35 compounds, rendering four further hits. The potency of these hit compounds was assessed in vivo using a Galleria mellonella larvae model infected with M. mycetomatis; the results were promising for several hits in terms of prolonged larval survival and/or reduced fungal burden. These results are the starting point of an Open Source Mycetoma (MycetOS) approach in which members of the global scientific community are invited to participate and contribute as equal partners.

Click here to read the article / PDF