title: Structure-activity relationship studies of antiplasmodial aminomethylthiazoles.
abstract: Structure-activity relationship (SAR) studies around a previously reported antimalarial aminomethylthiazole pyrazole carboxamide 1 are reported. Several analogues were synthesised and profiled for in vitro antiplasmodial activity against the drug-sensitive Plasmodium falciparum malaria parasite strain, NF54. Although all the reported analogues exhibited inferior in vitro antiplasmodial activity (IC50 = 0.125-173 μM) relative to compound 1 (IC50 = 0.0203 μM), one analogue, compound 5a, retained submicromolar activity (IC50 = 0.125 μM).
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Peter Mubanga
authors.initials: PM
authors.lastname: Cheuka
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Diego Gonzalez
authors.initials: DG
authors.lastname: Cabrera
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
authors.forename: Tanya
authors.initials: T
authors.lastname: Paquet
authors.affiliation: Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa. Electronic address: Kelly.Chibale@uct.ac.za.
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D051379:Mice; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000962:Antimalarials; D013844:Thiazoles
keywords: Aminomethylthiazoles; Antimalarial drug; Antiplasmodial activity; Structure–activity relationship; Thiazoles