gem-Dithioacetylated indole derivatives as novel antileishmanial agents.

Bioorg Med Chem Lett

Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India. Electronic address:

Published: October 2017

In this communication we report a serendipitously discovered hybrid molecule 1, combining fragment of 3 (an in vivo active antileishmanial molecule) with HS 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 12.5μg/ml without even deforming them (CC>100μg/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.

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http://dx.doi.org/10.1016/j.bmcl.2017.09.018DOI Listing

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gem-Dithioacetylated indole derivatives as novel antileishmanial agents.

Bioorg Med Chem Lett

October 2017

Medicinal & Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, UP, India. Electronic address:

In this communication we report a serendipitously discovered hybrid molecule 1, combining fragment of 3 (an in vivo active antileishmanial molecule) with HS donor moiety (known for bimodal behavior of cytoprotection and apoptosis), as antileishmanial agent. Compound 1 suppresses 99.82% parasitemia of L.

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