2. Academic Validation
  3. Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives

Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives

  • ACS Med Chem Lett. 2012 Nov 26;4(1):128-31. doi: 10.1021/ml300362a.
Matshawandile Tukulula 1,  Rajni-Kant Sharma 1,  Maïa Meurillon 1,  Aman Mahajan 1,  Krupa Naran 2,  Digby Warner 2,  Jianxing Huang 3,  Belew Mekonnen 3,  Kelly Chibale 4
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.
  • 2 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.
  • 3 Hager Biosciences LLC , 116 Research Drive, Suite 265, Bethlehem, Pennsylvania 18015, United States.
  • 4 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.
PMID: 24900574 DOI: 10.1021/ml300362a
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.

Keywords

Nitroimidazoles; antimycobacterial activity; antiplasmodial; nitroimidazooxazines.

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