title: Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity.
abstract: 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.
authors.affiliation: Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India.
authors.forename: Hardeep
authors.initials: H
authors.lastname: Kaur
authors.affiliation: Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisboa, Av. Prof. Egas Moniz, 1649-028 Lisboa, Portugal.
authors.forename: Marta
authors.initials: M
authors.lastname: Machado
authors.affiliation: Division of Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
authors.forename: Carmen
authors.initials: C
authors.lastname: de Kock
authors.affiliation: Division of Pharmacology, Department of Medicine, University of Cape Town, Observatory 7925, South Africa.
authors.forename: Peter
authors.initials: P
authors.lastname: Smith
authors.affiliation: Department of Chemistry, South African Medical Research Council Drug Discovery and Development Research Unit, Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 701, South Africa.
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
authors.affiliation: Instituto de Medicina Molecular, Faculdade de Medicina da Universidade de Lisboa, Av. Prof. Egas Moniz, 1649-028 Lisboa, Portugal.
authors.forename: Miguel
authors.initials: M
authors.lastname: Prudêncio
authors.affiliation: Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: kamaljit.chem@gndu.ac.in.
authors.forename: Kamaljit
authors.initials: K
authors.lastname: Singh
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008099:Liver / Q000187:drug effects* / Q000469:parasitology; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010962:Plasmodium berghei / Q000187:drug effects*; D011319:Primaquine / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D011743:Pyrimidines; C030986:pyrimidine; D011319:Primaquine
keywords: Antiplasmodial agents; Blood stage activity; Hybrid drugs; Liver stage activity; Primaquine; Pyrimidine