Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

gem-Dithioacetylated Indole Derivatives as Novel Antileishmanial Agents.

gem-Dithioacetylated Indole Derivatives as Novel Antileishmanial Agents.
In this communication we report a serendipitously discovered hybrid molecule 1, combining fragment of 3 (an in vivo active antileishmanial molecule) with H2S donor moiety (known for bimodal behavior of cytoprotection and apoptosis), as antileishmanial agent. Compound 1 suppresses 99.82% parasitemia of L. donovani infected macrophages at 12.5 μg/ml without even deforming them (CC50 > 100 μg/ml). This compound appears cytotoxic for intracellular amastigotes while cytoprotective to host macrophages. The concept can be utilized to develop high therapeutic index NCE (New Chemical Entities) for other macrophage mediated diseases like tuberculosis and cancer.

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17309034

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