title: Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives.
abstract: The synthesis and antiplasmodial and antimycobacterial evaluation of two new series of nitroimidazole and nitroimidazooxazine derivatives is described. The majority of these compounds, especially hybrids 9d, 9f, and 14b, exhibited potent activity against the chloroquine-resistant K1 strain of Plasmodium falciparum. Furthermore, a notable number from the tetrazole series were significantly more active against M. tuberculosis than kanamycin, a standard TB drug.
authors.affiliation: Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Matshawandile
authors.initials: M
authors.lastname: Tukulula
authors.affiliation: Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Rajni-Kant
authors.initials: RK
authors.lastname: Sharma
authors.affiliation: Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Maïa
authors.initials: M
authors.lastname: Meurillon
authors.affiliation: Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Aman
authors.initials: A
authors.lastname: Mahajan
authors.affiliation: MRC/NHLS/UCT Molecular Mycobacteriology Research Unit, DST/NRF Centre of Excellence for Biomedical TB Research, University of Cape Town , Rondebosch 7701, South Africa ; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Krupa
authors.initials: K
authors.lastname: Naran
authors.affiliation: MRC/NHLS/UCT Molecular Mycobacteriology Research Unit, DST/NRF Centre of Excellence for Biomedical TB Research, University of Cape Town , Rondebosch 7701, South Africa ; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
authors.forename: Digby
authors.initials: D
authors.lastname: Warner
authors.affiliation: Hager Biosciences LLC , 116 Research Drive, Suite 265, Bethlehem, Pennsylvania 18015, United States.
authors.forename: Jianxing
authors.initials: J
authors.lastname: Huang
authors.affiliation: Hager Biosciences LLC , 116 Research Drive, Suite 265, Bethlehem, Pennsylvania 18015, United States.
authors.forename: Belew
authors.initials: B
authors.lastname: Mekonnen
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.
authors.forename: Kelly
authors.initials: K
authors.lastname: Chibale
keywords: Nitroimidazoles; antimycobacterial activity; antiplasmodial; nitroimidazooxazines