1. Novel 4-[4-(4-methylpiperazin-1-yl)phenyl]-6-arylpyrimidine derivatives and their antitrypanosomal activities against T.brucei
- Author
-
Taylor, Annie E, Hering, Moritz, Elsegood, Mark RJ, Teat, Simon J, Weaver, George W, Arroo, Randolph RJ, Kaiser, Marcel, Maeser, Pascal, and Bhambra, Avninder S
- Subjects
Medicinal and Biomolecular Chemistry ,Chemical Sciences ,Infectious Diseases ,Vector-Borne Diseases ,Orphan Drug ,Rare Diseases ,Infection ,Good Health and Well Being ,Humans ,Trypanosoma brucei brucei ,Trypanosoma brucei rhodesiense ,Trypanosomiasis ,African ,Pyrimidines ,Trypanocidal Agents ,Parasitic Sensitivity Tests ,Molecular Structure ,Structure-Activity Relationship ,Dose-Response Relationship ,Drug ,Antiparasitic ,Antitrypanosomal ,Kinetoplastid ,Neglected tropical diseases ,T.brucei ,Organic Chemistry ,Pharmacology and Pharmaceutical Sciences ,Medicinal & Biomolecular Chemistry ,Medicinal and biomolecular chemistry ,Organic chemistry - Abstract
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
- Published
- 2024