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In Vitro Evaluation of the Antimalarial Activity of a Designed Novel Quinuclidine Derivative


Affiliations
1 Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India
2 CSIR-North East Institute of Science and Technology, Jorhat 785 006, India
 

A simple Schiff base, N-(pyridine-4-yl-methylene) quinuclidine-3-amine was synthesized from 3-amino-quinuclidine and 4-pyridine carboxaldehyde. The physico-chemical properties of the synthesized com-pound were studied. Molecular docking study was carried out and the quinuclidine derivative was evaluated for its in vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum strain. Although higher dose of synthesized compound was required for antimalarial activity (EC50 = 13.125 μg/ml) in comparison to chloroquine (EC50 5.144 μg/ml), the correlation coefficient confirmed good fit of the data. Furthermore, the result of the molecular docking provided insights into the ligand-protein interactions responsible for the inhibitory potency.

Keywords

Antimalarial, Docking, HPLC, Plasmodium falcipurum, Quinuclidine, Mass, NMR.
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  • In Vitro Evaluation of the Antimalarial Activity of a Designed Novel Quinuclidine Derivative

Abstract Views: 353  |  PDF Views: 121

Authors

Rupanjali Sharma
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India
Amrit Goswami
CSIR-North East Institute of Science and Technology, Jorhat 785 006, India
Mithun Rudrapal
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India
Dipsikha Sharma
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India
Hemanta Kumar Sharma
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India
Dipak Chetia
Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India

Abstract


A simple Schiff base, N-(pyridine-4-yl-methylene) quinuclidine-3-amine was synthesized from 3-amino-quinuclidine and 4-pyridine carboxaldehyde. The physico-chemical properties of the synthesized com-pound were studied. Molecular docking study was carried out and the quinuclidine derivative was evaluated for its in vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum strain. Although higher dose of synthesized compound was required for antimalarial activity (EC50 = 13.125 μg/ml) in comparison to chloroquine (EC50 5.144 μg/ml), the correlation coefficient confirmed good fit of the data. Furthermore, the result of the molecular docking provided insights into the ligand-protein interactions responsible for the inhibitory potency.

Keywords


Antimalarial, Docking, HPLC, Plasmodium falcipurum, Quinuclidine, Mass, NMR.



DOI: https://doi.org/10.18520/cs%2Fv111%2Fi12%2F2028-2030