Primaquine–pyrimidine hybrids: Synthesis and dual-stage antiplasmodial activity

• DOI: 10.1016/j.ejmech.2015.06.045
• Publication Date: 2015-07-02T14:12:55Z
• Authors: Hardeep Kaur; Marta Machado; Carmen de Kock; Peter Smith; Kelly Chibale; Miguel Prudêncio; Kamaljit Singh
• Keywords: Liver stage activity; Dose-Response Relationship, Drug; Molecular Structure; Plasmodium berghei; Antiplasmodial agents; Primaquine; Hybrid drugs; 01 natural sciences; Blood stage activity; Cell Line; 0104 chemical sciences; 3. Good health; Mice, Inbred C57BL; Antimalarials; Mice; Structure-Activity Relationship; Pyrimidines; Pyrimidine; Liver; Parasitic Sensitivity Tests; Animals; Humans

A series of novel pyrimidine-primaquine hybrids were synthesized and their effectiveness against the blood and liver stages of malaria parasites was evaluated. The hybrids displayed enhanced liver stage in vitro activity against P. berghei liver stage infection.