by Koovits PJ, Dessoy MA, Matheeussen A, Maes L, Caljon G, Ferreira LLG, Chelucci RC, Michelan-Duarte S, Andricopulo AD, Campbell S, Kratz JM, Mowbray CE, Dias LC. RSC Medicinal Chemistry 2020; doi: 10.1039/D0MD00165A
Summary: A series of benzene sulphonamides with good potency and selectivity against intracellular amastigotes of Leishmania spp. was identified by high-throughput screening. Approximately 200 compounds were synthesized as part of a hit-to-lead optimization programme. Ongoing detailed mode-of-action studies may provide an opportunity to use target-based medicinal chemistry to overcome issues with the current series. This article is part of a themed collection on neglected tropical diseases.
