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- W2953204044 abstract "1,4-Thiazepines derivatives are pharmacologically important heterocycles with different applications in medicinal chemistry. In the present work, we describe the preparation of new bicyclic thiazolidinyl-1,4-thiazepines 3 by reaction between azadithiane compounds and Michael acceptors. The reaction scope was explored and the yields were optimized. The activity of the new compounds was evaluated against Nippostrongylus brasiliensis and Caenorhabditis elegans as anthelmintic models and Trypanosoma brucei brucei. The most active compound was 3l, showing an EC50 = 2.8 ± 0.7 μM against T. b. brucei and a selectivity index >71." @default.
- W2953204044 created "2019-06-27" @default.
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- W2953204044 date "2019-01-01" @default.
- W2953204044 modified "2023-10-18" @default.
- W2953204044 title "Synthesis of bicyclic 1,4-thiazepines as novel anti-<i>Trypanosoma brucei brucei</i> agents" @default.
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- W2953204044 doi "https://doi.org/10.1039/c9md00064j" @default.
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