Journal of
Pharmacognosy and Phytotherapy

  • Abbreviation: J. Pharmacognosy Phytother.
  • Language: English
  • ISSN: 2141-2502
  • DOI: 10.5897/JPP
  • Start Year: 2009
  • Published Articles: 223

Full Length Research Paper

4-(ethyl-p-chlorophenylglycinylamino)-7-chloroquinoline: Synthesis and in vivo antimalaria evaluation

Habila J. D.1*, Habila N.2, Ndukwe I. G.1, Amupitan J. O.1, Nok A. J.2 and Shode F. O.3
1Department of Chemistry Ahmadu Bello University Zaria-Nigeria. 2Department of Biochemistry Ahmadu Bello University Zaria-Nigeria 3School of Chemistry University of Kwazulu-Natal Durban, South Africa.
Email: [email protected]

  •  Accepted: 21 September 2011
  •  Published: 31 December 2011

Abstract

4-amino-7-chloroquinoline derivative was synthesized and characterized using both1D and 2D nuclear magnetic resonance (NMR) techniques, with the application of correlation spectroscopy (COSY), nuclear overhauser enhancement spectroscopy (NOESY), heteronuclear multiple bond correlation (HMBC), heteronuclear single quantum coherence (HSQC), liquid chromatography-mass spectroscopy (LC-MS) and infra-red (IR) spectroscopy. The in vivo antimalaria activity of the compound against Plasmodium berghei berghei (Pbb) was assessed within 5 days (D5) of treatment. The antimalaria effect of JH7E evaluated at D30 shows a mean inhibition of parasitemia 46.32, 60.40 and 85.71% recorded on Pbb effected mice at 25, 50 and 100 mgKg-1body weight dosages respectively as compared to 97.04 and 94.40% curative rate obtained for artemisinin and chloroquine (Standard drugs) used as positive control. The results of the investigation showed that JH7E is a possible lead candidate for the development of antimalarial drug, because of its strong antimalarial activity against Pbb.

 

Key words: 4-amino-7-chloroquinoline, antimalaria, Plasmodium bergei bergei. Spectroscopy.