Synthesis and Antimalarial Properties of Three Substituted Trinitro-Tribenzylamine

Junior Kindala, Ezekiel Afolabi, Noel Wannang, Ukpe Ajima, Francis Agwom, Titilayo Johnson, Jean Kayembe, Pius Mpiana and Kalulu Taba
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Junior Kindala: 1Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria
Noel Wannang: Department of Pharmacology, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria
Titilayo Johnson: Department of Biochemistry, Faculty of Medical Sciences, University of Jos, Nigeria
Kalulu Taba: Department of Chemistry, Faculty of Sciences, University of Kinshasa, Congo-DR

Organic & Medicinal Chemistry International Journal, 2016, vol. 1, issue 3, 70-73

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).

Keywords: juniper publishers:Medicinal Chemistry; Biochemistry Journal; Pharmacology Journal; biochemical pharmacology; molecular pharmacology; biochemistry; open access journals; peer reviewed journals; Open Access; Journal of Molecular Biochemistry; International Research Journal of Pure and Applied Chemistry; World Journal of Biological Chemistry; Biochemistry and Analytical Biochemistry; Biochemistry & Physiology: Open Access; Molecular Biology International; Plant Biochemistry & Physiology; International Journal of Molecular Sciences; Journal of Clinical and Medical Genomics; Environmental Analytical Chemistry; Medicinal Chemistry; Juniper publishers reivews (search for similar items in EconPapers)
Date: 2016
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Persistent link: https://EconPapers.repec.org/RePEc:adp:jomcij:v:1:y:2016:i:3:p:70-73

DOI: 10.19080/OMCIJ.2016.01.555561

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