Novel 4-4-(4-methylpiperazin-1-yl)phenyl-6-arylpyrimidine derivatives and their antitrypanosomal activities against T.brucei

Human African trypanosomiasis, or sleeping sickness, is a neglected tropical disease caused by Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense and is invariably fatal unless treated. Current therapies present limitations in their application, parasite resistance, or require further c...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2024-09, Vol.109, p.129825
Main Authors: Taylor, Annie E, Hering, Moritz, Elsegood, Mark R J, Teat, Simon J, Weaver, George W, Arroo, Randolph R J, Kaiser, Marcel, Maeser, Pascal, Bhambra, Avninder S
Format: Article
Language:English
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Summary:Human African trypanosomiasis, or sleeping sickness, is a neglected tropical disease caused by Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense and is invariably fatal unless treated. Current therapies present limitations in their application, parasite resistance, or require further clinical investigation for wider use. Our work, informed by previous findings, presents novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives with promising antitrypanosomal activity. In particular, 32 exhibits an in vitro EC50 value of 0.5 µM against Trypanosoma brucei rhodesiense, and analogues 29, 30 and 33 show antitrypanosomal activities in the
ISSN:1464-3405
1464-3405
DOI:10.1016/j.bmcl.2024.129825