Probing benzothiadiazine-1, 1-dioxide ethylene glycol derivatives against Leishmania: synthesis and in vitro efficacy evaluation

摘要: Leishmaniasis is a vector-borne, parasitic disease affecting millions of people and animals worldwide. Current therapeutic options have proven to be ineffective in both treating the disease and preventing its spread. As a result, new drugs must be developed to effectively combat this disease. In this study, a series of 14 benzothiadiazine-1, 1-dioxide derivatives were synthesised to investigate their antileishmanial potential and cytotoxicity. Derivative 9, 2-(2-phenoxyethyl)-2H-benzo [e][1, 2, 4] thiadiazine-1, 1-dioxide, was identi ed as the most inhibitory compound as it was observed to moderately inhibit the growth of L. major (IC50 103 µM) and L. donovani (IC50 153 µM) promastigotes. However, in general, the series presented with low biological activity, which may be attributed to reduced target a nity and/or undesired cell culture protein binding.