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Tetrazole-based deoxyamodiaquines: Synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents

Tetrazole-based deoxyamodiaquines: Synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents

A series of new deoxyamodiaquine-based compounds was synthesized via the modified TMSN3-Ugi multi-component reaction and evaluated in vitro for antiplasmodial activity. The most potent compounds, 6b, 6c and 6j, showed IC50 values in the range of 6–77 nM against chloroquine-resistant K1- and W2-strai...

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Bibliographic Details
Main Authors: Tukulula, Matshawandile, Njoroge, Mathew, Mugumbate, Grace C., Gut, Jiri, Rosenthal, Philip J., Barteau, Samuel, Streckfuss, Judith, Heudi, Olivier, Kameni-Tcheudji, Jacques, Chibale, Kelly
Format: Article
Language:English
Published: Elsevier 2022
Subjects:
Antiplasmodial
Cytochrome P450
Deoxyamodiaquine
Pharmacokinetics
Multi-component reaction
Online Access:https://doi.org/10.1016/j.bmc.2013.06.067
http://hdl.handle.net/11408/4927
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https://doi.org/10.1016/j.bmc.2013.06.067
http://hdl.handle.net/11408/4927