We report the evaluation of a small library of azole-bisindoles for their antileishmanial potential, in terms of efficacy on promastigotes and intracellular amastigotes. Nine compounds showed good activity on MHOM/TN/80/IPT1 promastigotes with IC values ranging from 4 to 10 μM. These active compounds were also tested on human (THP-1, HEPG2, HaCaT, and human primary fibroblasts) and canine (DH82) cell lines. was selected as the best compound, with no quantifiable cytotoxicity in mammalian cells, to test the efficacy on intracellular amastigotes. significantly reduced the infection index of both human and canine macrophages with an effect comparable to the clinically used drug pentamidine. emerges as a new anti-infective agent with remarkable antileishmanial activity and no cytotoxic effects on human and canine cells.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8717589 | PMC |
http://dx.doi.org/10.1021/acsomega.1c05611 | DOI Listing |
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