Title:Synthesis of Metal Complexes of Primaquine and In-vitro Antimalarial Evaluation Against Plasmodium falciparum
Volume: 15
Issue: 6
Author(s): Rimmy Nandal, Aakash Deep*, Ishwar Singh, Meenakshi Kaushik, Hoti S. L., Balasubramanian Narasimhan, Rakesh K. Marwaha and Arun K. Sharma
Affiliation:
- Department of Pharmaceutical Sciences, Chaudhary Bansi Lal University, Bhwani 127021,India
Keywords:
Primaquine, metal complexes, antimalarial drugs, inflammation, morbidity, Plasmodium falciparum.
Abstract:
Background: Resistance to malarial drugs represents a major obstacle in the treatment of
disease, thereby increasing the need for more efficient drugs. The development of metal complexes
offers the medicinal chemist an opportunity to expand the activity of drugs. For providing supportive
therapy to the host to boost its immune system several new antimalarial drugs are being beneath research,
but sufficient information on their efficacy is yet not available.
Methods: In view of above, eight drug metal complexes (Ba (II), Ca (II), Zn (II), St (II), Hg (II), Fe
(III), Cu (II), Ni (II) of Sulfamethoxazole (SMX) and Primaquine were synthesized and in-vitro evaluated
for their antimalarial activity against malaria parasite Plasmodium falciparum by using fluorescence
based assay.
Result: The antimalarial activity of Nickel (EC50= 1.41µM) and Zinc (EC50=0.96µM) complexes have
shown tremendous activity as compared to the standard drug Primaquine (EC50=0.07µM). The structures
of all these newly synthesized derivatives were confirmed by spectral data (IR, 1H NMR, 13C
NMR and Mass spectrometry).
Conclusion: In conclusion, this study describes that the preparation and antimalarial evaluation of metal
complexes of primaquine and sulphamethoxazole. Evaluation of their possible biological activities such
as antimalarial activity was carried out and most of the synthesized compounds (Nickel and Zinc metal
complexes) showed the good activity as compared to the standard drug primaquine. Therefore the compounds
are appropriate candidates for more investigation and some more derivatives can be synthesized
to get an imminent into the structure activity relationship of these compounds to be employed as biologically
useful agents.
