In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series

by Van den Kerkhof M, Mabille D, Chatelain E, Mowbray CE, Braillard S, Hendrickx S, Maes L, Caljon G. International Journal for Parasitology: Drugs and Drug Resistance 2018, 8(1): 81-86, doi: 10.1016/j.ijpddr.2018.01.006.

Summary: Three new chemical series (bicyclic nitroimidazoles, aminopyrazoles and oxaboroles) were selected as potential new drug leads for leishmaniasis. Pharmacodynamics studies included both in vitro and in vivo efficacy, cross-resistance profiling against the current antileishmanial reference drugs, and evaluation of their cidal activity potential. The new lead series were shown to have cidal pharmacodynamic activity and an absence of cross-resistance with any of the current antileishmanial drugs, which opens possibilities for combination treatment to reduce the likelihood of treatment failures and drug resistance.

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