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Synthesis and Antimalarial Properties of Three Substituted Trinitro-Tribenzylamine

Author

Listed:
  • Junior Kindala

    (1Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria)

  • Ezekiel Afolabi
  • Noel Wannang

    (Department of Pharmacology, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria)

  • Ukpe Ajima
  • Francis Agwom
  • Titilayo Johnson

    (Department of Biochemistry, Faculty of Medical Sciences, University of Jos, Nigeria)

  • Jean Kayembe
  • Pius Mpiana
  • Kalulu Taba

    (Department of Chemistry, Faculty of Sciences, University of Kinshasa, Congo-DR)

Abstract

Malaria infection is a major health burdens in Tropical Africa and this is made worst with the emergence of Plasmodium falciparum resistance to the commonly used antimalarial drugs. There is therefore the need for new potent antimalarial drugs. Syntheses of o-trinitro tribenzylamine (2TBN), m-trinitro tribenzylamine (3TBN) and p-trinitro tribenzylamine (4TBN) were carried and yields of 38.49%, 41.01% and 39.67% respectively were obtained on reacting the respective o-, m-, and p-nitro benzaldehyde with formamide. The three synthesized trinitro-tribenzylamine derivatives were tested in vitro against Plasmodium falciparum isolates (3D7 strain) using parasite lactate dehydrogenase assay (pLDH). The result showed significant activity with IC50 ranging from 18 to 30 nM. The meta derivative (IC50:18.823 nM) showed better antiplasmodial activity than ortho (IC50: 30.287 nM) and para (IC50: 22.297 nM) derivatives, and even chloroquine phosphate (IC50: 22.777 nM).

Suggested Citation

  • Junior Kindala & Ezekiel Afolabi & Noel Wannang & Ukpe Ajima & Francis Agwom & Titilayo Johnson & Jean Kayembe & Pius Mpiana & Kalulu Taba, 2016. "Synthesis and Antimalarial Properties of Three Substituted Trinitro-Tribenzylamine," Organic & Medicinal Chemistry International Journal, Juniper Publishers Inc., vol. 1(3), pages 70-73, October.
    • Handle: RePEc:adp:jomcij:v:1:y:2016:i:3:p:70-73
    DOI: 10.19080/OMCIJ.2016.01.555561
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